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

…, KW Woods, A Claiborne, SL Gwaltney, KJ Barr…

Index: Li, Qun; Woods, Keith W.; Claiborne, Akiyo; Gwaltney, Ii, Stephen L.; Barr, Kenneth J.; Liu, Gang; Gehrke, Laura; Credo; Hui, Yu Hua; Lee, Jang; Warner, Robert B.; Kovar, Peter; Nukkala, Michael A.; Zielinski, Nicolette A.; Tahir, Stephen K.; Fitzgerald, Michael; Kim, Ki H.; Marsh, Kennan; Frost, David; Ng, Shi-Chung; Rosenberg, Saul; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 3 p. 465 - 469

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Citation Number: 76

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, ...