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Short Paper | Regular issue | Vol 83, No. 6, 2011, pp.1409-1415
Published online, 20th April, 2011
DOI: 10.3987/COM-11-12207
Synthesis of 12,12a-Dihydro-7,12a-diazacyclohepta[cd]benz[g]azulen-12-one (Cyclohepta[mn]pyrrolo[1,2-c][1,4]benzodiazepin-12-one) and Evaluation of Cytotoxic Activity against HeLa S3 Cells

Eiko Yoshioka, Hiroyuki Fujii, Toshihiro Murafuji, Reiko Ikeda, Takeo Konakahara, Takahiro Gunji, and Noritaka Abe*

*Department of Industrial Chemistry, Faculty of Science and Technology, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan


12,12a-dihydro-7,12a-diazacyclohepta[cd]benz[g]azulen-12-one (cyclohepta[mn]pyrrolo[2,1-c][1,4]benzodiazepin-12-one) derivative (7) was synthesized by the intramolecular cyclization of methyl 2-(3-phenyl-1-azaazulen-8-yl)aminobenzoate. Compound (7) showed extremely strong cytotoxic activity against HeLa S3 cells (IC50=0.543±0.063 μM).