Synthesis of indazole based diarylurea derivatives and their antiproliferative activity against tumor cell lines

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• 作者：Cui-rong Zhao^a ; Rui-qi Wang^a ; Gang Li^b ; Xiao-xia Xue^b ; Chang-jun Sun^b ; Xian-jun Qu^a ; ^{qxj@sdu.edu.cn} ; Wen-bao Li^b ; ^{wbli@sanlugen.com}
• 关键词：Indazole based diarylureas ; Antiproliferative activity ; Sorafenib
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 April, 2013
• 年：2013
• 卷：23
• 期：7
• 页码：1989-1992
• 全文大小：1914 K

文摘

New series of indazole based diarylureas were synthesized and their anticancer activity against cancer cells H460, A549, OS-RC-2, HT-29, Lovo, HepG2, Bel-7402, SGC-7901 and MDA-MB-231 were examined. These derivatives of diarylureas, except azaindazole based diarylureas 5f, 5l and 5m, showed superior or similar activity against most of these selected cancer cell lines to the reference compound sorafenib. The effect of substituents on the indazole ring was also investigated. Derivatives with trifluoromenthy or halogen substituent on the indazole ring showed higher activity against the selected cancer cell lines than sorafenib. The acute toxicity assay showed that compounds 5a, 5b and 5i possessed lower toxicity than sorafenib. Compound 5i with 4-(trifluoromenthy)-1H-indazole and 4-(trifluoromenthy) benzene moieties exhibited the most potent anticancer activity.