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