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Issue 37, 2019

Design and synthesis of novel phenylaminopyrimidines with antiproliferative activity against colorectal cancer

Author affiliations

Abstract

New phenylaminopyrimidine (PAP) derivatives have been designed and synthesised as potential tyrosine kinase inhibitors for the treatment of cancer. The synthesized compounds share a general structure and vary in the substitution pattern at position-2 of the pyridine ring. Several derivatives have demonstrated potent anticancer activities against HCT-116, HT-29 and LS-174T colorectal cancer cells. Furthermore, a number of hits showed good selectivity to Src-kinase. The cytotoxic mechanisms of these compounds were also investigated by studying their effects on cell-cycle distribution. Among all the compounds examined, compound 8b (with a terminal pyridin-3-yl moiety at the pyridine ring) showed the highest inhibitory selectivity towards src-kinase, which was coupled with cell cycle arrest, and apoptotic and autophagic interference, in colorectal cancer cells. This report introduces a novel category of PAP derivatives with promising kinase inhibitory and anticancer effects against colon cancer.

Graphical abstract: Design and synthesis of novel phenylaminopyrimidines with antiproliferative activity against colorectal cancer

Supplementary files

Article information


Submitted
05 May 2019
Accepted
04 Jul 2019
First published
11 Jul 2019

This article is Open Access

RSC Adv., 2019,9, 21578-21586
Article type
Paper

Design and synthesis of novel phenylaminopyrimidines with antiproliferative activity against colorectal cancer

H. A. Henidi, A. M. Al-Abd, F. A. Al-Abbasi, H. A. BinMahfouz and I. M. El-Deeb, RSC Adv., 2019, 9, 21578 DOI: 10.1039/C9RA03359A

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