The syntheses of neocryptolepine derivatives containing an amino acid or a dipeptide at the C-9 position, their evaluation for antitumor activity in vitro and in vivo were reported. To establish the influence of the amino acid or the peptide on the physicochemical properties of 5H-indolo[2,3-b]quinoline (DiMIQ), lipophilic and hemolytic properties were investigated. Most of the compounds displayed a high anticancer activity in vitro, and strongly inhibited growth of tumor in mice compared to cyclophosphamide. The attachment of the hydrophilic amino acid or peptide to the hydrophobic DiMIQ increased its hydrophilic properties, and decreased its hemotylic activity.

The glycylglycine conjugate (7a) was the most promising derivative. It strongly inhibited the growth of the tumor in mice (at dose 50mg/kg/day it inhibited the tumor growth by 46-63% on days 11^th-16^th, and by 29-43% on day 18^th-23^th), and significantly decreased hemolytic activity and lowered the in vivo toxicity compared to DiMIQ.

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