Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents

Bioorganic & Medicinal Chemistry
Huan-Qiu LiHai-Liang Zhu

Abstract

Two series of novel N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas (1a-18a; 1b-18b) as potential EGFR and HER-2 kinase inhibitors have been discovered. These compounds displayed good EGFR and HER-2 inhibitory activity and the SARs are also been studied. Especially compound 7b demonstrated significant EGFR and HER-2 inhibitory activity (IC(50)=0.08 microM for EGFR and IC(50)=0.35 microM for HER-2). Docking simulation was performed to position compound 7b into the EGFR active site to determine the probable binding conformation and antiproliferative assay results indicating that these series of urea and thioureas own high antiproliferative activity against MCF-7. Above all, thiourea 7b would be a potential anticancer agent deserves further research.

References

Apr 20, 1990·Cell·A Ullrich, J Schlessinger
Dec 30, 1994·Biochimica Et Biophysica Acta·N E Hynes, D F Stern
May 16, 2009·Anti-cancer Agents in Medicinal Chemistry·Huan-Qiu LiHai-Liang Zhu

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Citations

Oct 12, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Qing-Shan LiHai-Liang Zhu
Jan 7, 2014·Expert Opinion on Therapeutic Patents·Si-Ning Li, Huan-Qiu Li
Feb 18, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jingzi LiuBin He
Mar 16, 2013·Bioorganic & Medicinal Chemistry·Wen-Qun LiKuo-Hsiung Lee
Oct 12, 2012·Dalton Transactions : an International Journal of Inorganic Chemistry·Bhajan LalFazlul Huq
Nov 2, 2020·Bioorganic & Medicinal Chemistry Letters·Samia A ElseginySameh S M Soliman
Jul 3, 2021·Journal of Basic and Clinical Physiology and Pharmacology·Aguslina KirtishantiAristika Dinaryanti
Oct 4, 2014·Journal of Medicinal Chemistry·Molly A SilversGrover L Waldrop

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