Development of combretastatins as potent tubulin polymerization inhibitors |
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| Institution: | 1. School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430070, China;2. Department of Pharmaceutical Chemistry, College of Pharmacy, Aljouf University, Aljouf, Sakaka 2014, Saudi Arabia;1. University of Newcastle upon Tyne, School of Electrical and Electronic Engineering, Newcastle upon Tyne, UK;2. The Institute for Molecular Medicine, Huntington Beach, CA, USA;1. CompuNet, Istituto Italiano di Tecnologia, 16163 Genova, Italy;2. Laboratory of Biomolecular Research, Department of Biology and Chemistry, Paul Scherrer Institute, 5232 Villigen PSI, Switzerland;3. Department of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy;1. School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China;2. College of Pharmacy, University of Florida, Orlando, FL 32827, USA;3. Chengdu Easton Biopharmaceuticals Co., Ltd., Chengdu 611731, China;4. Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA;5. School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China;1. Department of Pharmacodynamics and Molecular Pharmacology, Faculty of Pharmacy, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland;2. Department of Inorganic and Analytical Chemistry, Faculty of Pharmacy, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland;3. Department and Institute of Nutrition and Dietetics, Faculty of Health Sciences, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland;4. Department and Clinic of Geriatrics, Faculty of Health Sciences, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland;5. Department of Histology and Embryology, Faculty of Medicine, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland;6. Faculty of Biotechnology, University of Wroclaw, Wrocław, Poland;7. Department of Chemical Technology of Drugs, Faculty of Pharmacy, Poznan University of Medical Sciences, Poznań, Poland;8. Department of Crystallography, Faculty of Chemistry, Adam Mickiewicz University, Poznań, Poland;1. Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123, Palermo, Italy;2. Net4Science srl, Academic spinoff, Università Magna Græcia di Catanzaro, Viale Europa, 88100, Italy;3. Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia di Catanzaro, Viale Europa, 88100, Italy;4. Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut, Forschungsstrasse 111, 5232, Villigen, PSI, Switzerland;5. University of Basel, Biozentrum, CH - 4056, Basel, Switzerland;6. Institute of Oncology Research, Faculty of Biomedical Sciences, USI, Via Francesco Chiesa 5, 6500, Bellinzona, Switzerland;7. Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, 21702, United States;8. Dipartimento di Scienze della Salute, Università Magna Græcia di Catanzaro, Viale Europa, 88100, Italy;9. Oncology Institute of Southern Switzerland, Ente Ospedaliero Cantonale, 6500, Bellinzona, Switzerland |
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| Abstract: | The combretastatins are isolated from South African tree combretum caffrum kuntze. The lead compound combretastatin A-4 has displayed remarkable cytotoxic effect in a wide variety of preclinical tumor models and inhibits tubulin polymerization by interacting at colchicine binding site of microtubule. However, the structural simplicity of C A-4 is favorable for synthesis of various derivatives projected to induce rapid and selective vascular shutdown in tumors. Majority of the molecules have shown excellent antiproliferative activity and are able to inhibit tubulin polymerization as well as possible mechanisms of action have been investigated. In this review article, the synthesis and structure-activity relationships of C A-4 and immense number of its synthetic derivatives with various modifications on the A, B-rings, bridge carbons and their anti mitotic activities are discussed. |
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| Keywords: | Combretastatin A-4 Anticancer Antiproliferative Isolation Natural products |
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