Synthesis and antitumor activity of novel cyclopropapyrroloindole (CPI) derivatives bearing bis(methoxycarbonyl) groups

✍ Scribed by Yasumichi Fukuda; Yasuo Oomori; Yoshie Kusama; Shiro Terashima

• Book ID: 104364911
• Publisher: Elsevier Science
• Year: 1997
• Tongue: English
• Weight: 255 KB
• Volume: 7
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(97)00099-1

✦ Synopsis

The title synthesis was achieved by employing oxidative cyclization of the enaminodiester prepared by Michael addition of the 5-aminoindoline with dimethyl acetylenedicarboxylate, as a key step. Some of these novel bis(methoxycarbonyl)cyclopropapyrroloindole (MC2CPI) derivatives 9c, d and their seco-chlorides 18c, d were found to exhibit prominent cytotoxicity and antitnmor activity against P388 murine leukemia.