Development of combretastatins as potent tubulin polymerization inhibitors

Bukhari Syed Nasir Abbas, Gajjela Bharath Kumar, Hrishikesh Mohan Revankar, Hua Li Qin

Research output: Contribution to journalReview article

15 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)130-147
Number of pages18
JournalBioorganic Chemistry
Volume72
DOIs
Publication statusPublished - 1 Jun 2017
Externally publishedYes

Fingerprint

Tubulin Modulators
Tubulin
Polymerization
Tumors
Combretum
Lead compounds
Derivatives
Colchicine
Structure-Activity Relationship
Microtubules
Blood Vessels
Neoplasms
Carbon
Binding Sites
Molecules
combretastatin

Keywords

  • Anticancer
  • Antiproliferative
  • Combretastatin A-4
  • Isolation
  • Natural products

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry

Cite this

Development of combretastatins as potent tubulin polymerization inhibitors. / Syed Nasir Abbas, Bukhari; Kumar, Gajjela Bharath; Revankar, Hrishikesh Mohan; Qin, Hua Li.

In: Bioorganic Chemistry, Vol. 72, 01.06.2017, p. 130-147.

Research output: Contribution to journalReview article

Syed Nasir Abbas, Bukhari ; Kumar, Gajjela Bharath ; Revankar, Hrishikesh Mohan ; Qin, Hua Li. / Development of combretastatins as potent tubulin polymerization inhibitors. In: Bioorganic Chemistry. 2017 ; Vol. 72. pp. 130-147.
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