Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives

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...

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Published inFuture medicinal chemistry Vol. 14; no. 14; pp. 1027 - 1048
Main Authors Kuzu, Burak, Hepokur, Ceylan, Turkmenoglu, Burcin, Burmaoglu, Serdar, Algul, Oztekin
Format Journal Article
LanguageEnglish
Published England 01.07.2022
Subjects
benzoxazole
phortress
molecular docking
cell-cycle
apoptosis
flow cytometry
cytotoxicity
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Summary: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. 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. Methyl 2-(thiophen-2-yl)benzo[d]oxazole-6-carboxylate ( ) has a higher effect than fluorouracil to induce apoptotic cell death (apoptosis value of 49.44%). Cell-cycle analysis shows that the compounds and methyl 2-(furan-2-yl)benzo[d]oxazole-6-carboxylate ( ) can be used as potential cell-cycle blockers by arresting MCF-7 cells in G0/G1 phase at rates of 63% and 85%, respectively.
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ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2022-0076