Cho, Hye Jung El-Gamal, Mohammed Ibrahim Oh, Chang-Hyun Lee, So Ha Sim, Taebo Kim, Garam Choi, Hong Seok Choi, Jung Hoon Yoo, Kyung Ho 2024-01-20T12:02:37Z 2024-01-20T12:02:37Z 2021-09-05 2013-07 0009-2363 https://pubs.kist.re.kr/handle/201004/127903 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, id, 1g, and 1j showed the highest potency against A375P cell line with IC50 values in sub-micromolar scale. In addition, compound id exerted high selectivity towards RAF1 serine/threonine kinase with 96.47% inhibition at 101 mu m, and IC50 of 0.961 mu m. This compound can possess antiproliferative activity against melanoma cells through inhibition of RAF1 kinase. English PHARMACEUTICAL SOC JAPAN THERAPEUTIC TARGET DERIVATIVES DIARYLAMIDES DIARYLUREAS Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAFI Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line Article 10.1248/cpb.c13-00283 1 CHEMICAL & PHARMACEUTICAL BULLETIN, v.61, no.7, pp.747 - 756 CHEMICAL & PHARMACEUTICAL BULLETIN 61 7 747 756 scie scopus 000321176500010 2-s2.0-84880029086 Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy Pharmacology & Pharmacy Chemistry Article THERAPEUTIC TARGET DERIVATIVES DIARYLAMIDES DIARYLUREAS bioisostere melanoma quinolinylaminoisoquinoline Sorafenib antiproliferative activity