Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
- Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
- 조혜정; 모하메드엘가말; 오창현; 이소하; 심태보; 김가람; 최홍석; 최정훈; 유경호
- bioisostere; melanoma; quinolinylaminoisoquinoline; Sorafenib; antiproliferative activity
- Issue Date
- Chemical & pharmaceutical bulletin
- VOL 61, NO 7, 747-756
- Design and synthesis of a new series of quinolinylaminoisoquinoline derivatives as conformationally restricted
bioisosteres of Sorafenib are described. Their in vitro antiproliferative activity against A375P melanoma
cell line was tested. Compounds 1b, 1d, 1g, and 1j showed the highest potency against A375P cell line
with IC50 values in sub-micromolar scale. In addition, compound 1d exerted high selectivity towards RAF1
serine/threonine kinase with 96.47% inhibition at 10 μM, and IC50 of 0.96 μM. This compound can possess
antiproliferative activity against melanoma cells through inhibition of RAF1 kinase.
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