Design, synthesis and cytotoxic evaluation of 4-anilinoquinazoline-triazole-AZT hybrids as anticancer agents

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Abstract

A series of 4-anilinoquinazoline-triazole-AZT hybrids were designed and synthesized as anticancer agents. Their cytotoxic potential has been evaluated by means of a micro-dilution assay against three human cancer cell lines (KB, epidermoid carcinoma; HepG2, hepatoma carcinoma; SK-Lu-1, non-small lung cancer). The biological results revealed that compounds 4b and 6d showed good anticancer activities against KB, HepG2, and Lu cell lines (IC50 values ranging from 9 µM to 100 µM). Especially, compounds 4b and 6d exhibited up to 3-fold more potent than reference drugs erlotinib hydrochloride and AZT in term of anti-lung cancer activity.

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Giang, L. N. T., Nga, N. T., Van, D. T., Anh, D. T. T., Phuong, H. T., Thanh, N. H., … Van Kiem, P. (2018). Design, synthesis and cytotoxic evaluation of 4-anilinoquinazoline-triazole-AZT hybrids as anticancer agents. Natural Product Communications, 13(12), 1633–1636. https://doi.org/10.1177/1934578x1801301215

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