Design, Synthesis and Cytotoxic Evaluation of 4-Anilinoquinazoline– triazole–AZT Hybrids as Anticancer Agents

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Design, Synthesis and Cytotoxic Evaluation of 4-Anilinoquinazoline– triazole–AZT Hybrids as Anticancer Agents

Giang, Le Nhat Thuy; Nga, Nguyen Thi; Van, Dinh Thuy; Anh, Dang Thi Tuyet; Phuong, Hoang Thi; Thanh, Nguyen Ha; Anh, Le Thi Tu; Trung, Vu Quoc; Van Tuyen, Nguyen; Van Kiem, Phan

Natural product communications, 12/2018, Volume: 13, Issue: 12

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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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