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Article Abstract
A series of eleven 4-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-]pyrimidines were designed and synthesized and their biological activities were evaluated. Synthesis involved the Gewald reaction to synthesize ethyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate ring, and SAr reactions. Compound was 1.6- and ~7-fold more potent than the lead compound in cell proliferation and microtubule depolymerization assays, respectively. Compounds , and showed the most potent antiproliferative effects (IC values < 40 nM), while compounds , , , and had lower antiproliferative potencies (IC values of 53-125 nM). Additionally, compounds -, and - circumvented Pgp and III-tubulin mediated drug resistance, mechanisms that diminish the clinical efficacy of paclitaxel (PTX). In the NCI-60 cell line panel, compound exhibited an average GI of ~10 nM in the 40 most sensitive cell lines. Compound demonstrated statistically significant antitumor effects in a murine MDA-MB-435 xenograft model.
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| http://dx.doi.org/10.3390/molecules27010321 | DOI Listing |
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