Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line

Title
Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
Authors
조혜정모하메드엘가말오창현이소하심태보김가람최홍석최정훈유경호
Keywords
bioisostere; melanoma; quinolinylaminoisoquinoline; Sorafenib; antiproliferative activity
Issue Date
2013-07
Publisher
Chemical & pharmaceutical bulletin
Citation
VOL 61, NO 7, 747-756
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/45830
ISSN
00092363
Appears in Collections:
KIST Publication > Article
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