Author: Aiden HempshallPublisher:
ISBN:
Category :
Languages : en
Pages : 530
Book Description
Novel Approaches to Isoform Selective Anti-cancer Drugs
Author: Aiden HempshallNew Approaches to Natural Anticancer Drugs
Author: Soodabeh SaeidniaPublisher: Springer
ISBN: 3319140272
Category : Medical
Languages : en
Pages : 117
Book Description
This book provides an up-to-date review of recently identified natural anti-tumor compounds from various natural origins including plants, fungi, endophytic fungi and marine organisms. It also includes discussion of new areas such as biotechnology and nanoparticles. Chapters explain the challenges and developments in anti-cancer drug discovery approaches, traditional remedies for prevention and treatment of cancer, marine-derived anti-cancer compounds, and antibiotics used as anti-cancer agents, as well as different classes of terpenoids and carbohydrates, which have been the subject of discussion in this field as efficient anti-cancer candidates. This book will be a concise guide for researchers in the field of pharmaceutical sciences, students and residents in pharmacy and medicine as well as those researching phytochemistry and natural products.
Anticancer Drug Discovery and Development: Natural Products and New Molecular Models
Author: Frederick A. ValeriotePublisher: Springer Science & Business Media
ISBN: 1461526108
Category : Medical
Languages : en
Pages : 289
Book Description
With the publication of these proceedings from the Second Drug Discovery and Development Symposium, this forum has become the main mechanism for bringing together the principal groups involved in both discovering and developing new approaches to the treatment of cancer. This Second Symposium emphasized the types of materials being discovered and their therapeutic activity. This is especially evident in the natural product discovery programs, where unique and active structures are being identified. The major contributors to the meeting were the investigators participating in the National Cooperative (Natural Products) Drug Discovery Groups [NC(NP)DDG]. These groups reflect an association among researchers at universities or cancer centers, pharmaceutical companies and the National Cancer Institute. Their sources of materials are varied, reflecting chemical inventories of pharmaceutical companies, organic synthetic compounds from the laboratory, cytotoxics as well as biologics and their hybrids, and natural products obtained from plants, marine organisms and microorganisms. The models employed in the discovery systems vary from broadly cellular based to specific enzymes to defined cellular functions. Each of them is believed important to the malignant state and will allow for the discovery of compounds which will have efficacy in cancer therapy. The goal of the participants is both to discover new anticancer agents and to develop them as efficiently as possible into clinically useful additions to treatment. Of importance is the fact that there are a number of promising leads which will soon be moving into the clinic thereby testing the effectiveness of this NC (NP) DDG approach.
Novel Anticancer Agents
Author: Alex A. AdjeiPublisher: Elsevier
ISBN: 0080537758
Category : Medical
Languages : en
Pages : 478
Book Description
Novel Anticancer Agents offers pertinent basic science information on strategies used for the rational design and discovery of novel anticancer agents, and, in addition, translational studies involving clinical trial design and execution with these novel, mostly cytostatic agents. This book covers basic science strategies that are being used in drug discovery and preclinical evaluation focused on novel molecular targets, as well as clinical trial methodology including clinical pharmacokinetics and imaging to address issues of efficacy evaluation of the new, relatively non-cytotoxic anticancer agents. At present, there is no book that provides such an integration of basic and clinical studies of novel anticancer agents, covering both drug discovery and translational research extensively. - Addresses the critical issues involved in the development of novel agents for cancer therapy by experts in the field - Presents drug discovery strategies - Discusses regulatory issues surrounding drug development
Novel approaches in anticancer drug design
Author: Design and Synthesis of Novel Anti-cancer Agents
Author: Ian RobinsonDesign, Synthesis, and Biological Evaluation of Novel Histone Deacetylase Inhibitors as Anti-cancer Agents
Author: Ayad Abed Ali Chiad Al-HamashiPublisher:
ISBN:
Category :
Languages : en
Pages : 305
Book Description
Despite major advances in cancer treatment strategies in recent years, significant limitations still remain. Selectively targeting cancer cells without affecting normal cells is a challenging task. Epigenetic modifications such as histone acetylation and methylation seem to play a crucial role in cancer pathophysiology. Histone acetylation is the most extensively studied epigenetic modification. Two groups of enzymes, histone deacetylases (HDACs) and histone acetyltransferases (HATs) control the acetylation status of histones. HDAC enzymes, which are overexpressed in many cancer tissues, provide a potential target for cancer chemotherapy. Therefore, HDAC inhibitors are currently being widely investigated as anticancer agents. Most of the current HDAC inhibitors are not selective and have toxic side effects. Selective inhibition of specific HDAC isoforms to preferentially suppress the proliferation of cancer cells is a goal yet to be achieved. Largazole is a macrocyclic, depsipeptide anticancer agent isolated from a marine cyanobacterium. It is a class I selective HDAC inhibitor. The depsipeptide cap group (CG) of largazole interacts with a less conserved area of the HDACs surface and can be targeted to develop isoform-selective HDAC inhibitors. We have used molecular modeling approaches to design several new largazole analogs with modified CGs to modulate the binding interaction with the enzyme surface. We used a novel protection/deprotection protocol to synthesize these analogs. The antiproliferative activity and HDAC isoform selectivity of the synthesized analogs were evaluated. The majority of the clinically used HDAC inhibitors are hydroxamates. Poor selectivity, poor pharmacokinetics, and severe toxic side effects are major limitations in their clinical use. There is a high need to develop new HDAC inhibitors with non-hydroxamate zinc binding groups (ZBG) with superior activity and selectivity profiles. We used molecular modeling studies to design a new class of HDAC inhibitors containing a 1-(1H-imidazol-2-yl)ethan-1-one (HIE) moiety as the ZBG. A structure-activity relationship (SAR) study was conducted by synthesizing a series of HIEs with different structural properties. Some of these compounds showed promising cell growth inhibition with GI50s in the upper nanomolar to lower micromolar range. A representative HIE compound inhibited purified HDAC enzymes with single digit micromolar IC50, with no selectivity preference among different HDAC isoforms. Replacing the ZBG with other groups such as 1-(thiazol-2-yl)ethan-1-one (TE), 1-(pyrimidin-2-yl)ethan-1-one (PE), and 1-(2-hydroxyphenyl)ethan-1-one (HPE) did not result in active compounds.
Targeted Therapies in Breast Cancer
Author: Gw SledgePublisher: Clinical Pub
ISBN: 9781846920660
Category : Breast
Languages : en
Pages : 0
Book Description
This new volume updates the reader on selected areas of targeted therapy in breast cancer, with special emphasis on chemoprevention strategies, drug resistance, biomarkers, combination chemotherapy, angiogenesis inhibition and pharmacogenomics in the context of clinical efficacy. This selected review of targeted therapies will guide the reader on effective treatment as part of an integrated programme of patient management.
Anticancer Agents from Natural Products
Author: Gordon M. CraggPublisher: CRC Press
ISBN: 9781420039658
Category : Medical
Languages : en
Pages : 628
Book Description
Plants, marine organisms, and microorganisms have evolved complex chemical defense and signaling systems that are designed to protect them from predators and provide other biological benefits. These organisms thus produce substances containing novel chemotypes that may have beneficial effects for humans. As collection methods improve and new screen
Anticancer Agents
Author: Qiao-Hong ChenPublisher: MDPI
ISBN: 3036501401
Category : Business & Economics
Languages : en
Pages : 606
Book Description
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.