Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2002 Feb 11;12(3):465-9.

Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.

Author information

1
Cancer Research, Abbott Laboratories, 60064-6101, Abbott Park, IL 60064-6101, USA. qun.li@abbott.com

Abstract

A series of indole containing oxazolines has been discovered as a result of structural modifications of the lead compound A-105972. The compounds exert their anticancer activity through inhibition of tubulin polymerization by binding at the colchicine site. A-289099 was identified as an orally active antimitotic agent active against various cancer cell lines including those that express the MDR phenotype. The anticancer activity, pharmacokinetics, and an efficient and enantioselective synthesis of A-289099 are described.

PMID:
11814821
DOI:
10.1016/s0960-894x(01)00759-4
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center