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Reevaluation of a Screening Program for Antineoplastic Agents

A total of 389 compounds and 40 antibiotics were active in the sequential screening program for antineoplastic agents at Lederle Laboratories during the past 8 years. Many of these compounds were folic acid antagonists, alkylating agents, or nicotinamide antagonists (thiadiazoles). The distribution of antineoplastic activity against the 3-tumor screen (Sarcoma 180, 6C3HED lymphosarcoma, and 72j mammary adenocarcinoma) was reviewed. Of the compounds, 78.4 and 10.3% were specifically active against the 72j tumor and the 6C3HED (Gardner) lymphosarcoma, respectively; 85 and 5% of the antibiotics were active against the 2 tumors. In contrast only 1% of the compounds and 2.5% of the antibiotics were specifically active against Sarcoma 180: azaserine, 2 folic acid antagonists, s-triazol-3-ylurea, and an antibiotic preparation. These 5 substances seemed like a small return for the effort expended in testing with Sarcoma 180 during the last 8 years. The importance of the 3 tumor types to the sequential screening program was further examined by reviewing the activity of 36 known carcinostatic compounds. Of these, 34 were active against either the 72j or the 6C3HED tumors or both. None of the 3 tumors detected vincaleukoblastine sulfate (VLB). Azaserine was the only substance which required Sarcoma 180 testing for detection. It was concluded that a sequential antineoplastic screening program with only the 72j and 6C3HED tumors would have found almost all the known compounds and all clinically useful compounds now detected by the 3-tumor screen.

¹ Department of Metabolic Chemotherapy, Lederle Laboratories Division, American Cyanamid Co., Pearl River, New York.