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A novel synthesis of benzo[c]phenanthridine skeleton and biological evaluation of isoquinoline derivatives.
Authors:W J Cho  M J Park  T Imanishi  B H Chung
Affiliation:College of Pharmacy, Chonnam National University, Kwangju, Korea.
Abstract:Benzo[c]phenanthridine skeleton was synthesized from easily available starting N-methyl-o-toluamide 2 and o-methylbenzonitrile 5 in 7 steps. Radical cyclization of styrene 10 afforded 6,11-dimethyl-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-5-one 13. Most 3-arylisoquinolines have displayed strong activities against human tumor cell lines. Especially, indenoisoquinolinone 13 exhibited excellent cytotoxicity (IC50 = 0.002 microgram/ml; HCT 15).
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