Synthesis and in‐vitro Cytotoxicity of Poly‐functionalized 4‐(2‐Arylthiazol‐4‐yl)‐4H‐chromenes |
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| Authors: | Majid Mahmoodi Alireza Aliabadi Saeed Emami Maliheh Safavi Saeed Rajabalian Mohammad‐Ali Mohagheghi Ahad Khoshzaban Alireza Samzadeh‐Kermani Navid Lamei Abbas Shafiee Alireza Foroumadi |
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| Institution: | 1. Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran;2. Cancer Research Center, Tehran University of Medical Sciences, Tehran, Iran;3. Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran. Fax: +98 21 664‐61178;4. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran;5. Research Laboratory, Iranian Tissue Bank Research & Preparation Center, Tehran University of Medical Sciences, Tehran, Iran |
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| Abstract: | A new series of 4‐aryl‐4H‐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‐4H‐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 IC50 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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| Keywords: | Apoptosis‐inducing agents 4‐Aryl‐4H‐chromenes Cytotoxic activity Thiazole |
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