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.

• Authors: W K Anderson, C P Chang, P F Corey, M J Halat, A N Jones, H L McPherson Jr, J S New, A C Rich
• Journal: Cancer treatment reports (Cancer Treat Rep) Vol. 66 Issue 1 Pg. 91-7 (Jan 1982) ISSN: 0361-5960 [Print] United States
• PMID: 7053273 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Pyrroles
• Pyrrolidines

Topics

• Animals
• Drug Evaluation, Preclinical
• Leukemia, Experimental (drug therapy)
• Male
• Mice
• Neoplasms, Experimental (drug therapy)
• Pyrroles (therapeutic use)
• Pyrrolidines (therapeutic use)
• Structure-Activity Relationship