1. Academic Validation
  2. Combination of 4-anilinoquinazoline and rhodanine as novel epidermal growth factor receptor tyrosine kinase inhibitors

Combination of 4-anilinoquinazoline and rhodanine as novel epidermal growth factor receptor tyrosine kinase inhibitors

  • Bioorg Med Chem. 2015 Jul 1;23(13):3221-7. doi: 10.1016/j.bmc.2015.04.065.
Si-Ning Li 1 Yun-Yun Xu 1 Jia-Yu Gao 1 Hong-Ran Yin 1 Shi-Lei Zhang 1 Huan-Qiu Li 2
Affiliations

Affiliations

  • 1 College of Pharmaceutical Science, Soochow University, Suzhou 215123, PR China.
  • 2 College of Pharmaceutical Science, Soochow University, Suzhou 215123, PR China. Electronic address: huanqiuli@suda.edu.cn.
Abstract

A type of novel rhodanine-based 4-anilinoquinazoline, which designed the combination between quinazoline as the backbone and various substituted biological rhodanine groups as the side chain, have been synthesized, and their antiproliferative activities were also evaluated firstly. These compounds displayed good antiproliferative activity and EGFR-TK inhibitory activity. Among them, compound 8d showed good inhibitory activity (IC50=2.7μM for Hep G2, IC50=3.1μM for A549) and molecular docking of 8d into EGFR TK active site was also performed, this inhibitor well fitting the active site might well explain its excellent inhibitory activity.

Keywords

4-Anilinoquinazoline; EGFR-TK inhibitors; Molecular docking; Rhodanine; Structure-based design.

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