Patent Evaluation: Bis-naphthalamides as antitumour agents

Summary

Novelty: Novel bis-naphthalamides are claimed to be useful antitumour agents. They are specifically stated to be effective against solid carcinomas.

Biology: In vitro assays were undertaken on murine leukaemia L1210 cells. ID₅₀ values were between 0.19 and 0.0025 mg/ml. In vivo tests were performed on transgenic mice with DLD-2 human colon tumours. The compounds are stated to have excellent activity.

Chemistry: Full preparative details are presented. Forty-three compounds are exemplified and eight compounds are specifically claimed, including (R,R)-2,2′-[1,2-ethamethylbis[imino(l-methyl-2,1-ethanediyl)]]-bis[5-nitro-lH-benz[de]isoquinoline-1,3-(2H)-dione].