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

Author:

Giang Le Nhat Thuy12,Nga Nguyen Thi2,Van Dinh Thuy2,Anh Dang Thi Tuyet12,Phuong Hoang Thi1,Thanh Nguyen Ha1,Anh Le Thi Tu1,Trung Vu Quoc3,Van Tuyen Nguyen12,Van Kiem Phan24

Affiliation:

1. Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

2. Graduate University of Science and Technology, VAST, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

3. Hanoi National University of Education, 136 Xuan Thuy, Cau Giay, Hanoi, Vietnam

4. Institute of Marine Biochemistry, VAST, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

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.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

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