Structure-activity relationships in antitumor aniline mustards.
Quantitative structure-activity relationships (QSAR) have been formulated for the hydrolysis of aniline mustards and their antitumor activity against Walker 256 tumor and L1210 and P388 leukemia. In general, the antitumor activity parallels hydrolysis under the conditions defined by Ross; toxicity (LD50) parallels antitumor efficacy. Chlorambucil is an exception. A most important finding is that ideal lipophilicity for effectiveness against Walker tumor appears to be much higher than for the leukemias which suggests that solid tumors may, in general, require more lipophilic drugs than leukemias.
D000816:Aniline Mustard / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D006868:Hydrolysis; D007928:Lethal Dose 50; D007939:Leukemia L1210 / Q000188:drug therapy; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D008954:Models, Biological; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D009588:Nitrogen Mustard Compounds; D000816:Aniline Mustard