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Synthesis and in-vitro Cytotoxicity of Poly-functionalized 4-(2-Arylthiazol-4-yl)-4H-chromenes

✍ Scribed by Majid Mahmoodi; Alireza Aliabadi; Saeed Emami; Maliheh Safavi; Saeed Rajabalian; Mohammad-Ali Mohagheghi; Ahad Khoshzaban; Alireza Samzadeh-Kermani; Navid Lamei; Abbas Shafiee; Alireza Foroumadi


Publisher
John Wiley and Sons
Year
2010
Tongue
English
Weight
906 KB
Volume
343
Category
Article
ISSN
0365-6233

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✦ Synopsis


Abstract

A new series of 4‐aryl‐4__H__‐chromenes bearing a 2‐arylthiazol‐4‐yl moiety at the 4‐position were prepared as potential cytotoxic agents. The in‐vitro cytotoxic activity of the synthesized 4‐aryl‐4__H__‐chromenes was investigated in comparison with etoposide, a well‐known anticancer drug, using MTT colorimetric assay. Among them, the 2‐(2‐chlorophenyl)thiazol‐4‐yl analog 4b showed the most potent activity against nasopharyngeal epidermoid carcinoma KB, medulloblastoma DAOY, and astrocytoma 1321N1, and compound 4d bearing a 2‐(4‐chlorophenyl)thiazol‐4‐yl moiety at the 4‐position of the chromene ring exhibited the best inhibitory activity against breast cancer cells MCF‐7, lung cancer cells A549, and colon adenocarcinoma cells SW480 with IC~50~ values less than 5 μM. The ability of compound 4b to induce apoptosis was confirmed in a nuclear morphological assay by DAPI staining in the KB and MCF‐7 cells.


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