2. Academic Validation
  3. 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

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

  • Eur J Med Chem. 2018 Jun 25:154:29-43. doi: 10.1016/j.ejmech.2018.05.006.
Yiqiang OuYang 1,  Wensheng Zou 1,  Liang Peng 1,  Zunhua Yang 2,  Qidong Tang 1,  Mengzi Chen 1,  Shuang Jia 1,  Hong Zhang 1,  Zhou Lan 1,  Pengwu Zheng 3,  Wufu Zhu 4
Affiliations

Affiliations

  • 1 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, China.
  • 2 College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • 3 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, China. Electronic address: zhengpw@126.com.
  • 4 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, China. Electronic address: zhuwufu-1122@163.com.
PMID: 29775935 DOI: 10.1016/j.ejmech.2018.05.006
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.

Keywords

Antiproliferative activity; EGFR inhibitors; Quinazoline derivatives; Synthesis.

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