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ID: ALA1135048
Journal: Bioorg Med Chem Lett
Title: 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.
Authors: Li Q, Woods KW, Claiborne A, Gwaltney SL, Barr KJ, Liu G, Gehrke L, Credo RB, Hui YH, Lee J, Warner RB, Kovar P, Nukkala MA, Zielinski NA, Tahir SK, Fitzgerald M, Kim KH, Marsh K, Frost D, Ng SC, Rosenberg S, Sham HL.
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.
CiteXplore: 11814821