Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives

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• 作者：Mohammed I. El-Gamal^a ; ^b ; ^c ; Mohammad Ashrafuddin Khan^d ; ^e ; Hamadeh Tarazi^a ; ^b ; Mohammed S. Abdel-Maksoud^d ; ^e ; ^f ; Mahmoud M. Gamal El-Din^d ; ^e ; ^f ; Kyung Ho Yoo^g ; Chang-Hyun Oh^d ; ^e ; ^{choh@kist.re.kr}
• 关键词：Antiproliferative activity ; C-RAF kinase ; Diarylurea ; Molecular docking ; Quinoline
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：413-423
• 全文大小：3307 K
• 卷排序：127

文摘

Synthesis and in vitro antiproliferative activities of new quinoline derivatives are reported. Compounds 1d-g were the most active and the most potent antiproliferative agents. Compounds 1e and 1g showed superior potency than Sorafenib. The IC50 of compounds 1e and 1g were in submicromolar scale against 18 cancer cell lines. IC50 of compound 1e against C-RAF kinase was 0.10 μM.