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

Abstract

A new series of phenylaminopyrimidine (PAP) derivatives was designed and synthesized to act against tyrosine kinases for the treatment of cancer.

Medicinal Chemistry Perspectives on Recent Advances in Src Kinase Inhibitors as a Potential Target for the Development of Anticancer Agents: Biological Profile, Selectivity, Structure‐Activity Relationship

“…The results explained that compound 30 was highly selective towards the Src kinase enzyme with EC 50 of 1.3 μM. This derivative showed hydrogen bond interactions with Gln278, Lys298, and Thr341 amino acids and steric interaction with Met344 and Ile339 residue of Src kinase [38] …”

“…This derivative showed hydrogen bond interactions with Gln278, Lys298, and Thr341 amino acids and steric interaction with Met344 and Ile339 residue of Src kinase. [38] Schoene et al designed and synthesized 2H-Indazoles candidates. These candidates had been screened as inhibitors of Src, Tie2 and SGK1.…”

Synthesis, Biological Evaluation, Molecular Docking and ADME Profiling of Methylpiperidin‐4‐ylphenyl‐nicotinamide Derivatives

“…Asciminib is a potent and selective allosteric ABL1 [20,21] inhibitor patented by Novartis Oncology [6,8] . Asciminib exhibited reduction in the side effects as compared to another TKI drug [10,23] basutinib. Various other approved CML drugs [11,12] have been discontinued after four years in use for cancer [7–9,19] treatment due to the problem of resistance which has arisen due to point mutations in BCR‐ABL [2,4,8,15,21] .…”

2-Chloro-3-cyano-4-nitrobenzyl pyridinium bromide as a potent anti-lung cancer molecule prepared using a single-step solvent-free method

“…[13][14][15] Phenyl amino pyrimidine and hydroxysubstituted phenyl amino pyrimidine showed a selective src kinase inhibitory response and excellent anticancer response against the HT29CRC and HCT-116 cell lines. 16 Mohammed et al reported on in vitro anti-proliferative studies of trimethoxy phenyl-substituted pyridine against the MCF7, HEPG-2 and HCT116 cancer cell lines. 4-Nitro-substituted trimethoxy phenyl pyridine showed a signicant anticancer response against the HCT116, HEPG-2 and MCF7 cancer cell lines compared with hydroxy-, methoxy-, methyl-substituted and chloro trimethoxy phenyl pyridine.…”