Abstract
The N 5–C 6 double bond of NK109 (an antitumor benzo[ c]phenanthridine alkaloid) is easily reduced under biological environment. To suppress the inactivation caused by reduction, we synthesized 5-, 6-, and 8-substituted NK109. 5-Substituted derivatives ( 4a– c) were reduced more easily than NK109. 6-Substituted ones ( 10a– f) inhibited biological reduction, but showed weak cytotoxic activity. 8 -O-Substituted ones ( 13a– h), especially 8- O-hydroxyethyl NK109 ( 13d), suppressed biological reduction and exhibited strong cytotoxic activity.
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