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5. Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors

Author

Hong Zhang, Yiqiang OuYang, Zunhua Yang, Pengwu Zheng, Wufu Zhu, Zhou Lan, Wensheng Zou, Chen Mengzi, Shuang Jia, Liang Peng, and Qidong Tang

Subjects
0301 basic medicine, Indoles, Afatinib, Antineoplastic Agents, Apoptosis, Pharmacology, 03 medical and health sciences, chemistry.chemical_compound, Structure-Activity Relationship, 0302 clinical medicine, Cell Line, Tumor, Drug Discovery, medicine, Humans, Propidium iodide, Protein Kinase Inhibitors, EGFR inhibitors, Cell Proliferation, Indole test, Dose-Response Relationship, Drug, Molecular Structure, Kinase, Organic Chemistry, Acridine orange, General Medicine, ErbB Receptors, Molecular Docking Simulation, 030104 developmental biology, chemistry, Docking (molecular), 030220 oncology & carcinogenesis, Drug Design, Quinazolines, Quinolines, Drug Screening Assays, Antitumor, medicine.drug
Abstract

Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ± 0.04 μM, 1.34 ± 0.13 μM and 1.23 ± 0.09 μM, respectively. Eight selected compounds were further selected to evaluated for the inhibitory activity against EGFR kinase. Three of them showed equal activity against EGFR kinase to positive control afatinib. AnnexinV-FITC, propidium iodide (PI) double staining and acridine orange single staining results indicated that the compound 13a could induce apoptosis of human lung cancer A549 cells.

Published
2018

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