Download or read book Synthetic Strategies for the Design of Platinum Anticancer Drug Candidates written by Justin Jeff Wilson and published by . This book was released on 2013 with total page 345 pages. Available in PDF, EPUB and Kindle. Book excerpt: (cont'd) Chapter 6. Synthesis, Characterization, and Cytotoxicity of Platinum(IV) Dicarbamate Complexes The reaction of cis,cis,trans-[Pt(NH3)2Cl2(OH)2] with alkyl and aryl isocyanates (RNCO) in DMF afforded dicarbamate complexes of the general formula cis,cis,trans- [Pt(NH 3)2Cl 2(O 2CNHR)2]. The resulting complexes were fully characterized by X-ray crystallography, multinuclear NMR spectroscopy, and cyclic voltammetry. The anticancer activities of these complexes were assessed in human lung cancer (A549) and human lung fibroblast (MRC-5) cell lines. Although no clear structure-activity relationships could be delineated, the complexes exhibited activity on the same order of magnitude as that of the clinically established drug cisplatin. Therefore, the reaction of cis,cis,trans-[Pt(NH3)2Cl 2(OH)2] with isocyanates provides a powerful new synthetic pathway to functionalize platinum(IV) anticancer agents. Appendix A. Aqueous Electrochemistry of a Platinum(IV) Prodrug Electrochemical studies of cis,cis,trans-[Pt(NH3)2Cl2(OAc) 2] in aqueous media were carried out. Cyclic voltammetry in pH 7.4 phosphate-buffered saline with glassy carbon and Pt disk working electrodes gave substantially different peak potentials for the irreversible reduction feature. Under these conditions, the glassy carbon electrode was plated with platinum metal derived from the platinum(IV) complex, as determined by cyclic voltammetry and chronoamperometry experiments. The bulk electrolysis of cis,cis,trans-[Pt(NH3)2Cl2(OAc)2] in aqueous solution at a carbon felt working electrode was investigated by 1H NMR spectroscopy. These studies indicate ligand loss upon reduction from both axial and equatorial sites of the platinum(IV) complex. Appendix B. Targeting the Mitochondria with Platinum Anticancer Agents using Mitochondria-Penetrating Peptides Early results of a collaborative effort with the lab of Professor Shana 0. Kelley at the University of Toronto to deliver platinum anticancer agents to the mitochondria are presented. Succinylacetone (Hsuccac) was used as a leaving group ligand for a cis-diammineplatinum(II) complex. The complex [Pt(succac)(NH 3)2](NO3), which contains a terminal, uncoordinated carboxylic acid functional group, was prepared and fully characterized. This complex was conjugated to a mitochondria-penetrating peptide (MPP) using standard solid-phase coupling chemistry. The anticancer activity of the Pt-MPP construct was tested in both wild-type and cisplatin-resistant ovarian cancer cell lines, A2780 and A2780CP70. Although less potent than cisplatin, the construct is equally toxic to both cell lines, thereby indicating that targeting the mitochondria provides a viable strategy for circumventing resistance to platinum drugs. Appendix C. Synthesis and Characterization of Several Novel Platinum Complexes Throughout the course of this thesis work, several platinum complexes were synthesized and characterized, but ultimately not fully pursued as potential anticancer agents. These species include platinum compounds with dichloroacetate, 2,2'-bis(1- methylimidazolyl)phenylmethoxymethane (BIPhMe), nitrogen mustard-containing, and nitroimidazole-derivatized ligands. The syntheses and characterization of these compounds are reported. Crystal structures are described for several of them.

Download or read book Anticancer Agents written by Qiao-Hong Chen and published by MDPI. This book was released on 2021-03-02 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Download or read book Structural and Functional Consequences of Platinum Anticancer Drug Binding to Free and Nucleosomal DNA written by Ryan Christopher Todd and published by . This book was released on 2010 with total page 229 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cisplatin, carboplatin, and oxaliplatin are three FDA-approved members of the platinum anticancer drug family. These compounds induce apoptosis in tumor cells by binding to nuclear DNA, forming a variety of adducts, and triggering cellular responses, one of which is the inhibition of transcription. The focus of this thesis is on studying the structure of these adducts, and correlating these effects with inhibition of transcription. Chapter 1 presents (i) a detailed review of the structural investigations of various Pt-DNA adducts and the effects of these lesions on global DNA geometry; (ii) research detailing inhibition of cellular transcription by Pt-DNA adducts; and (iii) a mechanistic analysis of how DNA structural distortions induced by platinum damage may inhibit RNA synthesis in vivo. These hypotheses will be explored in subsequent chapters of the thesis. In Chapter 2, features of the 2.17 A resolution X-ray crystal structure of cisdiammine(pyridine)chloroplatinum(II) (cDPCP) bound in a monofunctional manner to deoxyguanosine in a DNA duplex are discussed and compared to those of a cisplatin-1,2- d(GpG) intrastrand cross-link in double-stranded DNA. The global geometry of cDPCPdamaged DNA is quite different from that of DNA containing a cisplatin 1,2-d(GpG) cross-link. The latter platinated duplex is bent by ~40* toward the major groove at the site of the adduct; however, the monofunctional Pt-dG lesion causes no significant bending of the double helix. Like the cisplatin intrastrand adduct, however, the cDPCP moiety creates a distorted base pair step to the 5' side of the platinum site that may be correlated to its ability to destroy cancer cells. Structural features of monofunctional platinum adducts are analyzed, the results of which suggest that such adducts may provide a new platform for the design and synthesis of Pt anticancer drug candidates. The role of carbonate in the binding of cis-diamminedichloroplatinum(II) to DNA was investigated in Chapter 3 in order to understand the potential involvement of carbonato-cisplatin species in the mechanism of action of platinum anticancer agents. Cisplatin was allowed to react with single-stranded DNA in carbonate, phosphate, and HEPES buffers, and the products were analyzed by enzymatic digestion/mass spectrometry. The data from these experiments demonstrate (1) that carbonate, like other biological nucleophiles, forms relatively inert complexes with platinum that inactivate cisplatin, and (2) that the major cisplatin-DNA adduct formed is a bifunctional cross-link. These results are in accord with previous studies of cisplatin- DNA binding and reveal that the presence of carbonate has no consequence on the nature of the resulting adducts. The 1.77-A resolution X-ray crystal structure of a dodecamer DNA duplex with the sequence 5'-CCTCTGGTCTCC-3' that has been modified to contain a single engineered 1,2-cis- {Pt(NH 3)2}2+-d(GpG) cross-link, the major DNA adduct of cisplatin, is reported in Chapter 4. These data represent a significant improvement in resolution over the previously published 2.6-A structure. The ammine ligands in this structure are clearly resolved, leading to improved visualization of the cross-link geometry with respect to both the platinum center and to the nucleobases, which adopt a higher energy conformation. Also better resolved are the deoxyribose sugar puckers, which allow us to re-examine the global structure of platinum-modified DNA. Another new feature of this model is the location of four octahedral [Mg(H 20)6]2+ ion associated with bases in the DNA major groove and the identification of 124 ordered water molecules that participate in hydrogen bonding interactions with either the nucleic acid or the diammineplatinum(II) moiety. Chapter 5 discusses structural investigations of nucleosomal DNA modified by sitespecific platinum adducts. Nucleosome core particles containing a single 1,3-cis-{Pt(NH 3)2}2+_ d(GpTpG) intrastrand cross-link were synthesized and crystallized, and the X-ray structure was determined at 3.2 A resolution. The cisplatin adduct adopts a conformation facing toward the octamer core, in agreement with previous experiments. DNA in the vicinity of the Pt adduct has a similar helical bend as that observed in the NMR solution structure of free DNA containing the same cross-link, indicating that the rotational positioning power of cisplatin intrastrand crosslinks stems from the propensity to align the bent Pt-DNA structure with the DNA curvature arising from the nucleosome superhelix. Functional consequences of cisplatin binding to nucleosomal DNA are explored in Chapter 6. The effect of a single engineered platinum intrastrand cross-link on ATPindependent nucleosome mobility was investigated in vitro. Both 1,2-d(GpG) and 1,3-d(GpTpG) adducts of cisplatin inhibit translocation of DNA along the histone octamer, with the former Pt lesion providing a larger barrier. In vitro transcription assays with T7 RNA polymerase were conducted to determine whether cisplatin-DNA cross-links inhibit RNA synthesis by preventing access to nucleosomal DNA. Immobilized transcription templates containing a T7 RNAP promoter site, a single engineered cisplatin 1,2-d(GpG) or 1,3-d(GpTpG) intrastrand cross-link, and a phased nucleosome core particle were prepared. Analysis of resulting RNA transcript length revealed that the T7 RNAP elongation complex can overcome the energy barrier to nucleosome sliding caused by platinum intrastrand cross-links, but stalls when it reaches a Pt- DNA adduct placed on the DNA template strand. These results provide further evidence that intrastrand cross-links of cisplatin inhibit transcription by creating a physical barrier that the polymerase cannot pass. Appendices A and B summarize incomplete work that may be of use to future researchers working in this area. Appendix A describes attempts to isolate isomerically pure Pt- DNA probes containing a photoreactive benzophenone moiety, for use in cross-linking experiments that identify proteins that recognize and interact with cisplatin-DNA damage. In Appendix B efforts to obtain an X-ray crystal structure of an 1 Imer duplex DNA containing the 1,3- cis-{Pt(NH 3)2} 2 -d(GpTpG) intrastrand cross-link are reported. Appendix C details HPLC and mass spectrometric methods for purification and analysis of platinated oligonucleotides that were developed in the course of this research.

Download or read book Novel Strategies for Improving the Pharmacological Properties of Platinum acridine Anticancer Agents written by Song Ding and published by . This book was released on 2015 with total page 543 pages. Available in PDF, EPUB and Kindle. Book excerpt: Unlike traditional cisplatin-type platinum-based anticancer drugs, platinum-acridine hybrid agents were designed as dual platinating/intercalating DNA-targeted cytotoxics, which are able to cause cancer cell death at low-nanomolar concentrations. Unfortunately, the preclinical development of these agents has been hampered by their severe systemic toxicity. The goal of this dissertation was to devise strategies that improve the drug-like properties of platinum-acridines and allow their safe delivery. To achieve this, several classical and newly developed synthetic methodologies have been used to generate functionally unique hybrid agents. Several model systems, whole-cell assays, and animal studies have been used in this dissertation to validate their design and demonstrate their utility as anticancer agents. A modular screening platform was developed, based on a platinum-mediated amine-to-nitrile addition reaction, for rapid identification of functionalized platinum-acridine agents. These pre-screening assays produced functionalized "warheads" while providing insight into structure–activity relationships (SAR). Using several library members, we set out to explore synthetic approaches to construct platinum-acridine-based conjugates. A chemically robust azide-modified platinum-acridine was selected to validate the feasibility of copper-mediated and copper-free click chemistry as platinum-compatible conjugation reactions. This chemistry was used to attach fluorescent molecules to detect platinum-acridines in cancer cells by confocal microscopy. Both fluorophore tagging prior to incubation with cells and post-labeling methods were explored. In addition, a hydroxyl-modified warhead was conjugated with endoxifen via a chemically stable carbamate bond to produce a highly active hybrid agent in estrogen receptor positive (ER+) breast cancer. In another study, lipophilic ester-based prodrugs of platinum–acridines were generated showing improved drug-like properties (e. g., partition coefficients, logD). Two distinct pathways by which the target compounds can be activated have been confirmed by LC-ESMS and/or NMR techniques: (i) a platinum-assisted, self-immolative ester cleavage in a low-chloride environment, and (ii) enzymatic cleavage by human carboxylesterase-2 (hCES-2). Highly efficient amide coupling reactions in platinum complexes were also developed. This modular approach can be used to assemble a diverse library of platinum-acridines containing other bioactive components, such as molecularly targeted therapies, targeted ligands, and chemosensitizers. Finally, liposomal encapsulation of platinum-acridine was achieved, and the formulations were evaluated in A549 lung cancer xenograft models in mice. Improved anticancer efficacy of one of the liposomal formulations compared with the free drug was observed in this assay. In conclusion, the research in this dissertation has laid the foundation for the future preclinical development of platinum-acridines as oncology drugs by devising new synthetic methodology and providing proof-of-concept data in clinically relevant models of cancer.

Download or read book Anticancer Drug Development written by Bruce C. Baguley and published by Elsevier. This book was released on 2001-11-17 with total page 411 pages. Available in PDF, EPUB and Kindle. Book excerpt: Here in a single source is a complete spectrum of ideas on the development of new anticancer drugs. Containing concise reviews of multidisciplinary fields of research, this book offers a wealth of ideas on current and future molecular targets for drug design, including signal transduction, the cell division cycle, and programmed cell death. Detailed descriptions of sources for new drugs and methods for testing and clinical trial design are also provided. One work that can be consulted for all aspects of anticancer drug development Concise reviews of research fields, combined with practical scientific detail, written by internationally respected experts A wealth of ideas on current and future molecular targets for drug design, including signal transduction, the cell division cycle, and programmed cell death Detailed descriptions of the sources of new anticancer drugs, including combinatorial chemistry, phage display, and natural products Discussion of how new drugs can be tested in preclinical systems, including the latest technology of robotic assay systems, cell culture, and experimental animal techniques Hundreds of references that allow the reader to access relevant scientific and medical literature Clear illustrations, some in color, that provide both understanding of the field and material for teaching

Download or read book Biological Inorganic Chemistry written by Ivano Bertini and published by University Science Books. This book was released on 2007 with total page 794 pages. Available in PDF, EPUB and Kindle. Book excerpt: Part A.: Overviews of biological inorganic chemistry : 1. Bioinorganic chemistry and the biogeochemical cycles -- 2. Metal ions and proteins: binding, stability, and folding -- 3. Special cofactors and metal clusters -- 4. Transport and storage of metal ions in biology -- 5. Biominerals and biomineralization -- 6. Metals in medicine. -- Part B.: Metal ion containing biological systems : 1. Metal ion transport and storage -- 2. Hydrolytic chemistry -- 3. Electron transfer, respiration, and photosynthesis -- 4. Oxygen metabolism -- 5. Hydrogen, carbon, and sulfur metabolism -- 6. Metalloenzymes with radical intermediates -- 7. Metal ion receptors and signaling. -- Cell biology, biochemistry, and evolution: Tutorial I. -- Fundamentals of coordination chemistry: Tutorial II.

Download or read book Translocator Protein TSPO written by Giovanni Natile and published by MDPI. This book was released on 2018-03-05 with total page 177 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue "Translocator Protein (TSPO)" that was published in IJMS

Download or read book Bioconjugate Techniques written by Greg T. Hermanson and published by Academic Press. This book was released on 2010-07-26 with total page 1233 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bioconjugate Techniques, 2nd Edition, is the essential guide to the modification and cross linking of biomolecules for use in research, diagnostics, and therapeutics. It provides highly detailed information on the chemistry, reagent systems, and practical applications for creating labeled or conjugate molecules. It also describes dozens of reactions with details on hundreds of commercially available reagents and the use of these reagents for modifying or cross linking peptides and proteins, sugars and polysaccharides, nucleic acids and oligonucleotides, lipids, and synthetic polymers. A one-stop source for proven methods and protocols for synthesizing bioconjugates in the lab Step-by-step presentation makes the book an ideal source for researchers who are less familiar with the synthesis of bioconjugates More than 600 figures that visually describe the complex reactions associated with the synthesis of bioconjugates Includes entirely new chapters on the latest areas in the field of bioconjugation as follows: Microparticles and nanoparticlesSilane coupling agentsDendrimers and dendronsChemoselective ligationQuantum dotsLanthanide chelatesCyanine dyesDiscrete PEG compoundsBuckyballs,fullerenes, and carbon nanotubesMass tags and isotope tagsBioconjugation in the study of protein interactions

Download or read book Drug Monitoring and Clinical Chemistry written by Georg Hempel and published by Elsevier. This book was released on 2004-05-15 with total page 379 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug Monitoring and Clinical Chemistry, the 5th volume in the Handbook of Analytical Separations series, gives an overview about methods to analyse drugs in biological fluids. The most widely used methods to analyse drugs in biological fluids. i.e. chromatographic methods, CE and immunoassays are described in detail. For important drugs, an overview about the methods available and a comparison of the techniques should be given to enable the reader to choose the right method depending on laboratory equipment, staff, the aim of the investigation etc. Other general aspects important for conducting therapeutic drug monitoring or pharmacokinetics studies are also covered, i.e. sample preparation, validation of the analytical methods and pharmacokinetic methods for interpreting the data. Areas where therapeutic drug monitoring is used frequently such as antibiotics, immunosuppressant drugs, antipsychotic and anticancer drugs will be discussed in detail. In addition, the important field of phenotyping and genotyping for therapy optimisation with special focus on real-life applications is also covered. The book contains important information for analyst working on drug analysis in clinical chemistry, hospital pharmacists involved in therapeutic drug monitoring, other pharmacists, chemists or physicians working on pharmacokinetic studies in industry or academia. In contrast to other books in this field, this book provides up-to-date information regarding both methodology and clinical applications. For the applications, only fields are described where therapeutic drug monitoring is used in clinical routine and provides benefit to the patients. Overview of all important field where therapeutic drug monitoring is applied All relevant analytical and computational methods are discussed Written by experts with a lot of practical experience in the field

Download or read book Methods of Therapeutic Drug Monitoring Including Pharmacogenetics written by Georg Hempel and published by Elsevier. This book was released on 2019-10-17 with total page 380 pages. Available in PDF, EPUB and Kindle. Book excerpt: Methods of Therapeutic Drug Monitoring Including Pharmacogenetics, Second Edition, Volume Seven in the Handbook of Analytical Separations series, covers all aspects of drug monitoring, including laboratory work, pharmacokinetic analysis and clinical aspects, thus enabling readers from different fields to understand the whole process of therapeutic drug monitoring and how to avoid common pitfalls. The book contains analytical techniques for the quantification of drugs, along with pharmacogenetic and pharmacogenomic methods. Also included are updates on sample preparation, including dried blood spot technology and microextraction methods. In addition, the book includes new drugs, such as tyrosine kinase inhibitors and the monitoring of immunosuppressant drugs. Presents a unique, interdisciplinary approach that appeals to a wide range of users Written by authors from international labs, providing a global perspective that can be applied in various regulatory environments Features additional therapeutic drugs to reflect the rising number of immunocompromised patients Includes a new mass spectroscopic methods chapter to capture the frequent use in TDM and the improved availability of LC-MS across laboratories

Download or read book Cisplatin written by Bernhard Lippert and published by John Wiley & Sons. This book was released on 1999 with total page 628 pages. Available in PDF, EPUB and Kindle. Book excerpt: 30 years after its discovery as an antitumor agent, cisplatin represents today one of the most successful drugs in chemotherapy. This book is intended to reminisce this event, to take inventory, and to point out new lines of development in this field. Divided in 6 sections and 22 chapters, the book provides an up-to-date account on topics such as - the chemistry and biochemistry of cisplatin, - the clinical status of Pt anticancer drugs, - the impact of cisplatin on inorganic and coordination chemistry, - new developments in drug design, testing and delivery. It also includes a chapter describing the historical development of the discovery of cisplatin. The ultimate question - How does cisplatin kill a cell? - is yet to be answered, but there are now new links suggesting how Pt binding to DNA may trigger a cascade of cellular reactions that eventually result in apoptosis. p53 and a series of damage recognition proteins of the HMG-domain family appear to be involved. The book addresses the problem of mutagenicity of Pt drugs and raises the question of the possible relevance of the minor DNA adducts, e.g. of interstrand cross-links, and the possible use of trans-(NH3)2Pt(II)-modified oligonucleotides in antisense and antigene strategies. Our present understanding of reactions of cisplatin with DNA is based upon numerous model studies (from isolated model nucleobases to short DNA fragments) and application of a large body of spectroscopic and other physico-chemical techniques. Thanks to these efforts there is presently no other metal ion whose reactions with nucleic acids are better understood than Pt. In a series of chapters, basic studies on the interactions of Pt electrophiles with nucleobases, oligonucleotides, DNA, amino acids, peptides and proteins are reported, which use, among others, sophisticated NMR techniques or X-ray crystallography, to get remarkable understanding of details on such reactions. Reactivity of cisplatin, once bound to DNA and formerly believed to be inert enough to stay, is an emerging phenomenon. It has (not yet) widely been studied but is potentially extremely important. Medicinal bioinorganic chemistry - the role of metal compounds in medicine - has received an enormous boost from cisplatin, and so has bioinorganic chemistry as a whole. There is hardly a better example than cisplatin to demonstrate what bioinorganic chemistry is all about: The marriage between classic inorganic (coordination) chemistry and the other life sciences - medicine, pharmacy, biology, biochemistry. Cisplatin has left its mark also on areas that are generally considered largely inorganic. The subject of mixed-valance Pt compounds is an example: From the sleeping beauty it made its way to the headlines of scientific journals, thanks to a class of novel Pt antitumor agents, the so-called "platinum pyrimidine blues". In the aftermath diplatinum (III) compounds were recognized and studies in large numbers, and now an organometalic chemistry of these diplatinum (III) species is beginning to emerge. The final section of the book is concerned with new developments such as novel di- and trinuclear Pt(II) drugs with DNA binding properties different from those of cisplatin, with orally active Pt(IV) drugs which are presently in clinical studies, and with attempts to modify combinatorial chemistry in such a way that it may become applicable to fast screening of Pt antitumor drugs. The potential of including computational methods in solving questions of Pt-DNA interactions is critically dealt with in the concluding chapter.

Download or read book Metallo Drugs Development and Action of Anticancer Agents written by Astrid Sigel and published by Walter de Gruyter GmbH & Co KG. This book was released on 2018-02-05 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: Volume 18, entitled Metallo-Drugs: Development and Action of Anticancer Agents of the series Metal Ions in Life Sciences centers on biological, medicinal inorganic chemistry. The serendipitous discovery of the antitumor activity of cis-diamminodichloroplatinum(II) (cisplatin) by Barnett Rosenberg in the 1960s is a landmark in metallodrug-based chemotherapy. The success of cisplatin in the clinic, followed by oxaliplatin and carboplatin, along with their drawbacks relating mainly to resistance development and severe toxicity, initiated research on polynuclear platinum complexes and on Pt(IV) complexes as prodrugs. Furthermore, the indicated shortcomings led to the exploration of other transition and main group metal ions, among them Ru(II/III), Au(I/III), Ti(IV), V(IV/V), and Ga(III) including also the essential metal ions Fe(II/III), Cu(I/II), and Zn(II). Ionic as well as covalent and non-covalent interactions between structurally very different complexes and biomolecules like nucleic acids, proteins, and carbohydrates are studied and discussed with regard to their possible anticancer actions. Hence, MILS-18 summarizes the research at the forefront of medicinal inorganic chemistry, including studies on the next-generation, tailor-made anticancer drugs. All this and more is treated in an authoritative and timely manner in the 17 stimulating chapters of this book, written by 39 internationally recognized experts from 10 nations (from the US via Europe to China and Australia). The impact of this vibrant research area is manifested by more than 2700 references, nearly 150 illustrations (more than half in color) and several comprehensive tables. Metallo-Drugs: Development and Action of Anticancer Agents is an essential resource for scientists working in the wide range from enzymology, material sciences, analytical, organic, and inorganic biochemistry all the way through to medicine including the clinic ... not forgetting that it also provides excellent information for teaching.

Download or read book Advances and Prospects of 3d Metal Based Anticancer Drug Candidates written by Farukh Arjmand and published by Springer Nature. This book was released on with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. Presents information in a clear and concise way using a large number of figures Historical background provides insights on how the process of drug discovery in the anticancer field has evolved Extensive references to primary literature

Download or read book Metal based Anticancer Agents written by Angela Casini and published by Royal Society of Chemistry. This book was released on 2019-04-05 with total page 370 pages. Available in PDF, EPUB and Kindle. Book excerpt: Metal-based anticancer drugs are among the most successful therapeutic agents, as evidenced by the frequent prescription of selected platinum and arsenic compounds to patients. Metal-based Anticancer Agents covers the interdisciplinary world of inorganic drug discovery and development by introducing the most prominent compound classes based on different transition metals, discussing emerging concepts and enabling methods, as well as presenting key pre-clinical and clinical aspects. Recent progress on the unique features of next-generation targeted metal-based anticancer agents, including supramolecular coordination complexes used for both therapy and drug delivery, promise a bright future beyond the benefits of pure cytotoxic activity. With contributions from global leaders in the field, this book will serve as a useful reference to established researchers as well as a practical guide to those new to metallodrugs, and postgraduate students of medicinal chemistry and metallobiology.

Download or read book Advances in Metallodrugs written by Shahid Ul-Islam and published by John Wiley & Sons. This book was released on 2020-07-08 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is organized into 12 important chapters that focus on the progress made by metal-based drugs as anticancer, antibacterial, antiviral, anti-inflammatory, and anti-neurodegenerative agents, as well as highlights the application areas of newly discovered metallodrugs. It can prove beneficial for researchers, investigators and scientists whose work involves inorganic and coordination chemistry, medical science, pharmacy, biotechnology and biomedical engineering.

Download or read book Unconventional Anticancer Metallodrugs and Strategies to Improve their Pharmacological Profile written by Maria Contel and published by MDPI. This book was released on 2019-10-01 with total page 204 pages. Available in PDF, EPUB and Kindle. Book excerpt: For the past 40 years, metal-based drugs have been widely used for the treatment of cancer. Cisplatin and follow-up drugs carboplatin (ParaplatinTM) and oxaliplatin (EloxatinTM) have been the gold standard for metallodrugs in clinical settings as antineoplastic agents. While effective, these drugs (either alone or in combination therapy) have faced a number of clinical challenges resulting from their limited spectrum of activity, high toxicity leading to significant side effects, resistance, poor water solubility, low bioavailability and short circulating time. In the past 10 years, various unconventional non-platinum metal-based agents have emerged as a potential alternative for cancer treatment. These compounds are highly effective and selective in cancers resistant to cisplatin and other chemotherapeutic agents. Research in this area has recently exploded with a relevant number of patents and clinical trials, in addition to reports in scientific journals. Furthermore, in parallel to the synthesis of coordination and organometallic compounds comprising many different metals and unconventional platinum-based derivatives, researchers are focused on optimizing mechanistic and pharmacological features of promising drug candidates. This Special Issue aims to highlight the latest advances in anticancer metallodrugs with a focus on unconventional anticancer agents, as well as novel activation, targeting and delivery strategies aimed at improving their pharmacological profile.