Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives
Date
2022Metadata
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Background: Phortress produces reactive electrophilic metabolites that form DNA adducts only in
sensitive tumor cells. The authors converted the 2-phenylbenzothiazole nucleus in phortress to 2-
aryl and -heteroaryl benzoxazole derivatives (11 new and 14 resynthesized). All synthesized
compounds were studied for antitumor activity in various cancer cells. Materials & methods:
Cytotoxicity, cell morphology, flow cytometry and cell-cycle analyses of compounds were
performed and more active derivatives were tested in the MCF-7 cell line. Conclusion: Methyl 2-
(thiophen-2-yl)benzo[d]oxazole-6-carboxylate (BK89) has a higher effect than fluorouracil to
induce apoptotic cell death (apoptosis value of 49.44%). Cell-cycle analysis shows that the
compounds BK89 and methyl 2-(furan-2-yl)benzo[d]oxazole-6-carboxylate (BK82) can be used
as potential cell-cycle blockers by arresting MCF-7 cells in G0/G1 phase at rates of 63% and 85%,
respectively.