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- Title
Synthesis, Characterization, Crystal Structure, and Antitumor Activity of 2-Phenylthiazole–Coumarin Derivatives.
- Authors
Chen, K. Q.; Song, M. Q.; Wu, W. L.; Xia, X. S.; Hong, J. H.; Yang, S.; Qian, J. J.; Yang, Q.; Zou, J. P.; Shi, D. H.
- Abstract
2-(4-Methoxyphenyl)-1,3-thiazole4-carboxylic acid was synthesized by condensation, alkylation, and saponification reactions using 4-hydroxythiobenzamide and ethyl 3-bromopyruvate as raw materials. It was then reacted with α,ω-dibromoalkanes to obtain ω-bromoalkyl 2-(4-methoxyphenyl)-1,3-thiazole-4-carboxylates which were condensed with 7-hydroxycoumarins. The structure of the synthesized ω-(2-oxo-2H-chromen-7-yloxy)alkyl 2-(4-methoxyphenyl)-1,3-thiazole-4-carboxylates was confirmed by IR, NMR, and mass spectra and single crystal X-ray diffraction. Their antiproliferation activity against MCF-7 and cisplatin-resistant MCF-7/DDP human breast cancer cell lines was evaluated by using CCK-8 assay. All compounds showed some inhibitory effect at a concentration of 50 µM, and two compounds were found to be potent on both cancer cell lines.
- Subjects
ANTINEOPLASTIC agents; INHIBITORY Concentration 50; CRYSTAL structure; MASS spectrometry; CELL lines; CISPLATIN
- Publication
Russian Journal of Organic Chemistry, 2022, Vol 58, Issue 9, p1341
- ISSN
1070-4280
- Publication type
Article
- DOI
10.1134/S1070428022090214