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• W4281663510 endingPage "114493" @default.
• W4281663510 startingPage "114493" @default.
• W4281663510 abstract "A series of novel 2,4-diarylaminopyrimidine analogues (G-1∼G-8 and I-1∼I-24) were rationally designed by incorporating 2-alkyl-3-acyl-1H-indol fragment to interact with the hydrophobic region of the intractable ALKG1202R mutant. Wherein, compound I-24 bearing a 2-methyl-3-dimethylformamido-1H-indol moiety was identified as the most promising ALK inhibitor with IC50 values below 4 nM against ALKWT, ALKL1196M and ALKG1202R, accompanied by concrete down-regulation of phospho-ALK and its relative downstream signaling. Subsequently, I-24 displayed significant anti-proliferative activity in the nanomolar range towards ALK-positive cell lines including a panel of Ba/F3 cells harboring mutational ALK. Dramatically, the involvement of I-24 decreased colony formation and migration tendency on H2228 cells. Meanwhile, flow cytometry analysis indicated that I-24 could induce cell apoptosis and achieve cell cycle arrest in G1 phase. Notably, oral administration of I-24 at 50 mg/kg regressed tumor in the H2228 xenograft model with tumor growth inhibition value of 93.5%. Collectively, I-24 with favorable PK profile was supposed to further investigation as potent ALK inhibitor to circumvent clinical drug resistance." @default.
• W4281663510 created "2022-06-13" @default.
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• W4281663510 date "2022-08-01" @default.
• W4281663510 modified "2023-09-27" @default.
• W4281663510 title "Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants" @default.
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• W4281663510 doi "https://doi.org/10.1016/j.ejmech.2022.114493" @default.
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