Novel indolizino[8,7-b]indole hybrids as anti-small cell lung cancer agents: Regioselective modulation of topoisomerase II inhibitory and DNA crosslinking activities

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• 作者：Sue-Ming Chang^a ; Wilson Christian^a ; ^b ; Ming-Hsi Wu^a ; Tai-Lin Chen^a ; ^c ; Yi-Wen Lin^a ; Ching-Shu Suen^a ; Hima Bindu Pidugu^a ; Dilip Detroja^a ; ^b ; Anamik Shah^b ; Ming-Jing Hwang^a ; Tsann-Long Su^a ; ^{tlsu@ibms.sinica.edu.tw} ; Te-Chang Lee^a ; ^{bmtcl@ibms.sinica.edu.tw}
• 关键词：Anti-SCLC hybrids ; β-carboline ; bis(hydroxymethyl)pyrrole ; indolizino[8 ; 7-b]indole ; DNA cross-linking ; Topoisomerase inhibition
• 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：235-249
• 全文大小：2622 K
• 卷排序：127

文摘

Indolizino[8,7-b]indoles are hybrids of β-carboline and bis(hydroxymethyl)pyrrole. Hybrids inhibit Topo II and cause DNA cross-linking. N11-substituent affects two adjacent OH on pyrrole and DNA cross-linking activity. These hybrids induced cell arrest at the G2/M phase and apoptosis in cancer cells. 17a is more effective than etoposide and cisplatin against H526 SCLC xenografts.