Combretastatin A4 (CA4) is an antitumor compound isolated from the African bush willow tree (Combretum caffrum).1) CA4 binds to tubulin dimers and inhibits microtubule polymerization, thereby inducing mitotic arrest and apoptosis in endothelial cells.1,2) Combretastatin A4 phosphate disodium salt (CA4P), a water-soluble prodrug of CA4, is converted to CA4 by metabolism.3) It has been reported that CA4P has significant effects on tumor vascularization by disrupting vascular endothelial cadherin.4,5) Recently CA4 was also extracted from Brazilian Combretaceae family plant (Combretum leprosum).6) And various CA4 analogs have been synthesized and evaluated for antitumor activity.7,8)
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Antitumor Compound present in a Tree of Africa
References
- 1)Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4
- 2)Antineoplastic Agents. 291. Isolation and Synthesis of Combretastatins A-4, A-5, and A-6
- 3)Antineoplastic agents. 322. Synthesis of combretastatin A-4 prodrugs
- 4)Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues
- 5)Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial-cadherin signaling
- 6)Determination of Combretastatin A-4 in Combretum leprosum
- 7)Medicinal chemistry of combretastatin A4: Present and future directions
- 8)Combretastatin A-4 analogs as anticancer agents
