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Synthesis and in‐vitro Cytotoxicity of Poly‐functionalized 4‐(2‐Arylthiazol‐4‐yl)‐4 H ‐chromenes
Author(s) -
Mahmoodi Majid,
Aliabadi Alireza,
Emami Saeed,
Safavi Maliheh,
Rajabalian Saeed,
Mohagheghi MohammadAli,
Khoshzaban Ahad,
SamzadehKermani Alireza,
Lamei Navid,
Shafiee Abbas,
Foroumadi Alireza
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900198
Subject(s) - cytotoxicity , chemistry , cytotoxic t cell , mtt assay , dapi , in vitro , stereochemistry , moiety , cancer cell , cell culture , apoptosis , biochemistry , biology , cancer , genetics
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.