Structural modifications to develop olivacine analogs with reduced cross-resistance and side effects resulted in the discovery of S 16020-2. This drug showed a very potent cytotoxic effet in vitro and high therapeutic antitumor activity in vivo. 60% of P388-bearing mice were cured following the administration of 60 mg/kg/day (with an intermittent schedule) x3. The drug was still significantly active against the resistant P388/VCR model while adriamycin was totally inactive. Three intermittent injections of 40 mg/kg induced 100% cure in established Lewis lung carcinoma. Xenografts of human H-69 small cell lung carcinoma and H460 non small cell lung carcinoma were significantly sensitive to S 16020-2. These properties deserve further pharmacotoxicological studies. Keywords :