Journal
JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
Volume 8, Issue 4, Pages 983-991Publisher
SPRINGER
DOI: 10.1007/BF03246554
Keywords
Imidazole; 1,8-Acridinedione; Cytotoxicity; Calcium channel antagonist activity
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Funding
- Tehran University of Medical Sciences (TUMS)
- University of Tehran (TU)
- Iran National Science Foundation (INSF)
- Medicinal and Natural Product Chemistry Research Center, Shiraz, Iran
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A series of novel imidazolyl derivatives of fully and partially hydrogenated 1,8-acridinediones were synthesized and assessed for their cytotoxic activity on four different human cancer cell lines (HeLa, MCF-7, LS-180, and Raji cells). Although being inactive on LS-180 and Raji cell lines, the compounds showed weak to moderate anti-tumor activities on other cell lines and their IC50 ranged from 31.7 to more than 100 mu M. Among the synthesized compounds 12b, 13b, 12c and 13c, bearing an electron-attracting substituent on the imidazole ring, and 12f and 13f, with a benzyl substituent, showed higher activities. Furthermore, the calcium channel antagonist activity of the derivatives, an undesired effect when these compounds are used as anti-tumor agents, was much lower than that of Nifedipine, a reference antagonist. Imidazolyl derivatives of 1,8-acridinedione represent an interesting template, showing promising biological properties. Further investigation on this chemical scaffold could potentially lead to the discovery of cytotoxic agents with low calcium channel blocking activity.
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