title: Vinylogous carbinolamine tumor inhibitors. 8. Activity of bis(acyloxymethyl) derivatives of pyrroles and pyrrolizines against a panel of murine leukemias and solid tumors.
abstract: The activity of three pyrroles and four pyrrolizines is compared in several different experimental leukemias and solid tumors in mice. Two compounds were particularly noteworthy, the bis(N-cyclohexylcarbamate) and the bis[N-(2-propyl)] derivatives of 2,3-dihydro-5-(3,4-dichlorophenyl)-6,7-bis(hydroxymethyl)-1H-pyrrolizine. These two compounds showed a very high level of activity against B16 melanocarcinoma, CD8F1 mammary tumor, colon tumor 26, and colon tumor 38, and a significant number of "cures" were recorded. The isopropyl compound was more potent than the cyclohexyl compound, but both showed a similar profile of activity.
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical; D007942:Leukemia, Experimental / Q000188:drug therapy; D008297:Male; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D011758:Pyrroles / Q000627:therapeutic use*; D011759:Pyrrolidines / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
chemical_list: D011758:Pyrroles; D011759:Pyrrolidines