Novel indole-bearing combretastatin analogues as tubulin polymerization inhibitors.

ABSTRACT:

Background

The combretastatins are a class of natural stilbenoids. These molecules generally share three common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituent often at C3' and C4', and an ethene bridge between the two rings, which provides necessary structural rigidity. Members of the combretastatin family possess varying ability to cause vascular disruption in tumors. Combretastatin binds to the colchicine binding site of β-subunit of tubulin. Despite having a similar name, combretastatin is unrelated to statins, a family of cholesterol-lowering drugs.

Results

New combretastatin 2-(1-acetyl-1H-indole-3-yl)-3-(phenyl) propenoic analogues (2a to 2y), bearing indole moiety at the place of ring A of combretastatin (CA4), were synthesized and evalu

SUBMITTER: Kumar S 

PROVIDER: S-EPMC3599526 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature