2-Haloethylating agents for cancer chemotherapy. 2-Haloethyl sulfonates
- 1 August 1983
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 26 (8) , 1168-1173
- https://doi.org/10.1021/jm00362a016
Abstract
Because certain (2-chloroethyl)triazenes and (2-haloethyl)nitrosoureas have high antineoplastic activity, 2-chloroethyl and 2-fluoroethyl sulfonates were prepared to try to develop additional types of 2-haloethylating agents. Antineoplastic activity much superior to that of the prototype, 2-chloroethyl methanesulfonate, was found among 2-chloroethyl sulfonates. Among a variety of 2-chloroethyl alkane- and arenesulfonates, several substituted methanesulfonates displayed significant activity against P388 leukemia in mice; the chloromethanesulfonate showed high activity (T/C = 218%). None of the arenesulfonates were active in this test.This publication has 6 references indexed in Scilit:
- Chemistry of nitrosoureas. Intermediacy of 4,5-dihydro-1,2,3-oxadiazole in 1,3-bis(2-chloroethyl)-1-nitrosourea decompositionJournal of Medicinal Chemistry, 1980
- Mechanism of action of 2-haloethylnitrosoureas on DNA and its relation to their antileukemic propertiesBioorganic Chemistry, 1978
- INTERSTRAND CROSS-LINKING OF DNA BY 1,3-BIS(2-CHLOROETHYL)-1-NITROSOUREA AND OTHER 1-(2-HALOETHYL)-1-NITROSOUREAS1977
- A chemical basis for the antitumor activity of chloroethylnitrosoureasBiochemical Pharmacology, 1976
- The Modes of Decomposition of 1,3-Bis(2-chloroethyl)-1-nitrosourea and Related CompoundsJournal of Medicinal Chemistry, 1967
- The Synthesis of Potential Anticancer Agents. XXXVI. N-Nitrosoureas.1 II. Haloalkyl DerivativesJournal of Medicinal Chemistry, 1966