HOME
*





Combretastatin A4
Combretastatin A-4 is a combretastatin and a stilbenoid. It can be isolated from ''Combretum caffrum'', the Eastern Cape South African bushwillow tree or in ''Combretum leprosum'', the mofumbo, a species found in Brazil. Function Tubulin represents a potent target in cancer chemotherapy, given its role in cell division. Combretastatin is a naturally occurring well known tubulin polymerization inhibitor. Combretastatin A-4 comes in two stereoisomers (cis (shown top right), and trans); The cis form binds much better to the 'colchicine' site on tubulin to inhibit polymerization. Derivatives 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, including beta-lactam based compounds. See also * Ombrabulin Ombrabulin was an experimental drug candidate discovered by Ajinomoto and further dev ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  




Combretastatin A-1
Combretastatin A-1 is a combretastatin and a stilbenoid. It can be found in '' Combretum caffrum'', the Eastern Cape South African Bushwillow tree. Biological effects in mammals It is an antiangiogenic agent acting by destabilizing tubulin, which induces cell apoptosis of proliferating endothelial cells. Derivatives as drugs Currently designated an orphan drug by the FDA, combretastatin A1 diphosphate (OXi4503 or CA1P) is in Phase I clinical trials for relapsed and refractory acute myeloid leukemia and myelodysplastic syndrome A myelodysplastic syndrome (MDS) is one of a group of cancers in which immature blood cells in the bone marrow do not mature, and as a result, do not develop into healthy blood cells. Early on, no symptoms typically are seen. Later, symptoms may .... References Combretastatins Stilbenoids {{Aromatic-stub ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Combretastatin A-4
Combretastatin A-4 is a combretastatin and a stilbenoid. It can be isolated from '' Combretum caffrum'', the Eastern Cape South African bushwillow tree or in '' Combretum leprosum'', the mofumbo, a species found in Brazil. Function Tubulin represents a potent target in cancer chemotherapy, given its role in cell division. Combretastatin is a naturally occurring well known tubulin polymerization inhibitor. Combretastatin A-4 comes in two stereoisomers (cis (shown top right), and trans); The cis form binds much better to the 'colchicine' site on tubulin to inhibit polymerization. Derivatives 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, including beta-lactam A beta-lactam (β-lactam) ring is a four-membered lactam. A ''lactam'' is a cyclic amide, and ''beta''-lactams are named so be ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Combretastatin B-1
Combretastatin B-1 is a combretastatin and a dihydrostilbenoid Dihydrostilbenoids (bibenzyls) are natural phenols formed from the dihydrostilbene ( bibenzyl) backbone. Examples Dihydro-resveratrol is a natural phenol with a bibenzyl structure found in wine. It is also a metabolite of trans-resveratrol for .... It can be found in '' Combretum caffrum'', the Eastern Cape South African bushwillow tree or in '' Combretum kraussii'', the forest bushwillow.Uteroactive constituents from Combretum kraussii. Bridget K Brookes, Olga V Doudoukina, Lynn C Katsoulis and Joy H D Veale, South African Journal of Chemistry, Dec 99, Vol. 52, Issue 4, page 127abstract It can be produced by selective hydrogenation of Combretastatin A-1. It is a potent inhibitor of microtubule assembly in vitro. References Combretastatins Dihydrostilbenoids {{aromatic-stub ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Combretum
''Combretum'', the bushwillows or combretums, make up the type genus of the family Combretaceae. The genus comprises about 272 species of trees and shrubs, most of which are native to tropical and southern Africa, about 5 to Madagascar, but there are others that are native to tropical Asia, New Guinea and the Bismarck Archipelago, Australia, and tropical America. Though somewhat reminiscent of willows (''Salix'') in their habitus, they are not particularly close relatives of these. Ecology Bushwillow trees often are important plants in their habitat. Savannahs in Africa, in particular those growing on granitic soils, are often dominated by ''Combretum'' and its close relative ''Terminalia''. For example, ''C. apiculatum'' is a notable tree in the Angolan mopane woodlands ecoregion in the Kunene River basin in southern Africa. Other species of this genus are a major component of Southwestern Amazonian moist forests. This genus contains several species that are pollinated by ma ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]