Tubulin binding agents are an important class of antitumor agents and the most extensively studied binding sites are those that accommodate taxanes, vinca alkaloids and colchicine. Antimicrotubule disrupting agents like paclitaxel have major limitations against multidrug resistance (MDR) tumors. Overexpression of P-glycoprotein (Pgp) and/or �III-tubulin can severely limit their clinical utility as cancer chemotherapeutic agents. Recently, we reported substituted monocyclic N-methyl-4-methoxyanilino pyrimidines that are structurally simplified, conformationally flexible analogs of bicyclic pyrrolo[3,2-d]pyrimidines that circumvent some of the drawbacks of taxanes and vinca akaloids. Compounds 1-5  were designed to evaluate further the SAR at the 6-position of the pyrimidine scaffold. The design, synthesis and structure activity relationship of these agents with respect to their antitubulin activity will be presented.

Design, synthesis, and biological evaluation of substituted monocyclic pyrimidines with potential antitubulin activities as antitumor agents

248th National Meeting (2014)

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