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 in | Future medicinal chemistry Vol. 14; no. 14; pp. 1027 - 1048 |
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| Main Authors | , , , , |
| Format | Journal Article |
| Language | English |
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England
01.07.2022
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| Abstract | 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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| AbstractList | 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. |
| Author | Turkmenoglu, Burcin Hepokur, Ceylan Burmaoglu, Serdar Algul, Oztekin Kuzu, Burak |
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