Synthesis of Combretastatin A-4 Analogs and their.
Herein, we describe the design, synthesis and evaluation of the cytotoxicity of a series of novel Combretastatin A-4 derivatives. Furthermore, the most active of these compounds, CA-4E, was selected to investigate the antitumor mechanism of this novel series of compounds.
This paper reviews the most important approaches in analogs of combretastatin synthesis and presents structure-reactivity relationships for these compounds. Krystyna Dzierzbicka Keywords: Combretastatin A-4, CA-4, Inhibitors of angiogenesis, Synthesis; Biological activity, Cancer therapy.
Synthesis of combretastatin A-4 prodrugs ', Anti-Cancer Drug Design, vol. 10, no. 4, pp. 299-309. Pettit G, Temple C, Narayanan VL, Varma R, Simpson MJ, Boyd MR et al. Antineoplastic agents 322. Synthesis of combretastatin A-4 prodrugs.
We describe the design, synthesis, biochemical evaluation, and molecular modelling studies of a series of analogues of the microtubule-destabilising agent, combretastatin A-4 (CA-4).
Combretastatin A-4 is a tubulin-binding chemotherapy drug that is structurally related to colchicine (91). This drug was discovered and isolated from the African bush willow, Combretum caffrum. The more soluble phosphate form is cleaved by endogenous phosphatases to the original compound, which is then taken up into cells.
Synthesis of combretastatin analogs: evaluation of in vitro anticancer activity and molecular docking studies. Medicinal Chemistry Research 2012, 21 (11), 3720-3729.
Both combretastatin A-1 and combretastatin B-1 are potent inhibitors of microtubule assembly in vitro and among the most potent inhibitors of the binding of colchicine to tubulin yet described. The structural simplicity and ready synthesis of combretastatin A-1 and combretastatin B-1 suggest that these new biosynthetic products will become useful in a variety of biological endeavors.
Combretastatin A-1 is also a potent cytotoxic agent. Another molecule is combretastatin B-1. Biological function In the plants that make it. It is thought to help protect the plant from pests and parasites. In mammalian tumours. Members of the combretastatin family possess varying ability to cause vascular disruption in tumors.
Synthesis of Combretastatin A-4 Analogs and their Biological Activities Author(s): Agnieszka Siebert, Monika Gensicka, Grzegorz Cholewinski, Krystyna Dzierzbicka.
Synthesis and pharmacological evaluation of combretastatin-A4 analogs of pyrazoline and pyridine derivatives as anticancer, anti-inflammatory and antioxidant agents. Medicinal Chemistry Research 2018, 27 (4), 1226-1237.
This study is based on the synthesis of a series of combretastatin analogs with different substitutions on one aryl moiety and a carboxylic group in connecting chain. Cis-configuration with respect to aryl groups was established by X-ray crystal analysis.
Combretastatin A-4 is the active component of combretastatin A-4 phosphate, a prodrug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. A large number of synthetic derivatives have been reported, (5) (6) including beta-lactam based compounds.
This thesis covers work investigating the design, synthesis and evaluation of Combretastatin A-4 like chalcones and their analogues, and other anticancer agents. The first two chapters are an introduction to cancer chemotherapy and the development of tubulin as a target for chemotherapy. Chapter one includes information on cancer epidemiology, the history of cancer and the development of.
