Synthesis of nitrosourea derivatives of pyridine and piperidine as potential anticancer agents
- 1 August 1980
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 23 (8) , 848-851
- https://doi.org/10.1021/jm00182a007
Abstract
Nitrosourea derivatives 18-22 which utilize either a piperidine or pyridine ring as a carrier group were synthesized and evaluated for anticancer activity. N''-(1-Benzyl-4-piperidinyl)-N-(2-chloroethyl)-N-nitrosourea hydrogen maleate (19) exhibited good activity against intracranial [mouse] L1210 leukemia and the mouse ependymoblastoma brain tumor system. Compound 19 exhibited comparable activity in the [mouse] Lewis lung carcinoma system to N,N''-bis(2-chloroethyl)-N-nitrosourea. Replacement of the N-benzyl group in the 3-piperidinyl- and 4-piperidinylnitrosoureas resulted in less active compounds in all tumor systems tested. The 3-pyridylnitrosourea 22 was inactive in the L-1210 leukemia system.This publication has 1 reference indexed in Scilit:
- The Synthesis of Potential Anticancer Agents. XXXVI. N-Nitrosoureas.1 II. Haloalkyl DerivativesJournal of Medicinal Chemistry, 1966