Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives
Özet
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.
Anahtar kelimeler
Sürdürülebilir Kalkınma Amaçları
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SKA 3: Sağlıklı Bireyler
Atıf için künye
Kuzu, B., ÖZSOY, C., TÜRKMENOĞLU, B., Burmaoğlu, S., & ALGÜL, Ö. (2022). Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives. Future Medicinal Chemistry, 14(14), 1027–1048. https://doi.org/10.4155/fmc-2022-0076
BibTeX
@article{kuzu2022-79086,
author = {Kuzu, Burak and ÖZSOY, CEYLAN and TÜRKMENOĞLU, BURÇİN and Burmaoğlu, Serdar and ALGÜL, ÖZTEKİN},
title = {Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives},
journal = {Future Medicinal Chemistry},
year = {2022},
volume = {14},
number = {14},
pages = {1027--1048},
issn = {1756-8919},
doi = {10.4155/fmc-2022-0076},
url = {https://akademik.atauni.edu.tr/yayinlar/79086-design-synthesis-and-in-vitro-antiproliferation-activity-of-some-2-aryl-and}
}