Английская Википедия:Combretastatin A-4

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Шаблон:Chembox 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.[1][2]

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.[3]

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.Шаблон:Cn

A large number of synthetic derivatives have been reported,[4][5] including beta-lactam based compounds.[6]

See also

  • Ombrabulin, a combretastatin A-4 derivative in clinical trials for treatment of cancer

References

Шаблон:Reflist

Шаблон:Stilbenes

  1. Determination of Combretastatin A-4 in Combretum leprosum. SCN Queiroz, MR Assalin, S Nobre, IS Melo, RM Moraes, VL Ferracini and AL Cerdeira, Planta Med, 2010, volume 76, pages 53, Шаблон:Doi
  2. Шаблон:Cite journal
  3. Structural Basis of cis- and trans-Combretastatin Binding to Tubulin. Gaspari. 2017
  4. Шаблон:Cite journal
  5. Шаблон:Cite journal
  6. Шаблон:Cite journal