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Issue 37, 2019
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Design and synthesis of novel phenylaminopyrimidines with antiproliferative activity against colorectal cancer

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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

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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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