2-Chloroethyl (methylsulfonyl)methanesulfonate and related (methylsulfonyl)methanesulfonates. Antineoplastic activity in vivo.

doi:10.1021/JM00371A019

Paper

2-Chloroethyl (methylsulfonyl)methanesulfonate and related (methylsulfonyl)methanesulfonates. Antineoplastic activity in vivo.

Published May 1, 1984 · Y. Shealy, C. A. Krauth, W. Laster

Journal of medicinal chemistry

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21

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Abstract

2-Haloethyl and ethyl (methylsulfonyl)methanesulfonates were prepared via sulfene intermediates. 2-Chloroethyl (methylsulfonyl)methanesulfonate is highly active against P388 leukemia in vivo; the majority of leukemic mice treated with this compound at 50 mg/kg per day, qd 1-5, survived more than 30 days and about 37% survived for more than 60 days. 2- Fluoroethyl (methylsulfonyl)methanesulfonate is also highly effective against P388 cells in vivo, but it is more toxic. Other (methylsulfonyl)methanesulfonate esters are more active than the analogous methanesulfonates and chloromethanesulfonates .

Study Snapshot

2-Chloroethyl (methylsulfonyl)methanesulfonate shows promising anti-leukemic activity, with potential for clinical use in treating P388 leukemia.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

2-Chloroethyl (methylsulfonyl)methanesulfonate and related (methylsulfonyl)methanesulfonates. Antineoplastic activity in vivo.

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References

Citations

A Rational for Novel Anti-NeuroOncology Drugs

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Synthesis and Antineoplastic Evaluation of α-Substituted Alkanesulfonates: Analogues of Clomesone

Clomesone is more effective than its analogues in curing P388 leukemia, but the synthesis of clomesone has been simplified to one step from methanesulfonyl chloride.

Pre-clinical evaluation of a novel chloroethylating agent, Clomesone.

Clomesone showed no significant in vitro activity against solid human colorectal carcinomas and showed limited in vivo activity against murine tumors, suggesting it was not more selective than chloroethylnitrosoureas.

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