Chemotherapeutic Activity of New 2-Chloroethylnitrosoureas in Rat L5222 Leukemia: Comparison of Bifunctional and Water-Soluble Derivatives With 1,3-Bis(2-chloroethyl)-1-nitrosourea

1 February 1978

journal article
research article
Published by Oxford University Press (OUP) in JNCI Journal of the National Cancer Institute

Vol. 60 (2) , 345-348
https://doi.org/10.1093/jnci/60.2.345

Abstract

The chemotherapeutic activity of eight nitrosourea derivatives was compared with that of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in transplantable rat leukemia L5222 cells. Bifunctional 1,1′-polymethylenebis-3-(2-chloroethyl)-3-nitrosoureas effected cure rates between 30 and 75% in single equitoxic doses in the therapy of advanced ip implanted L5222 [staging of L5222 leukemia development (hr before median day of death in controls): early=<120; advanced=120-61; late=60-25; and preterminal= 24-0). Of three water-soluble monofunctional alkylatlng 1-(ω-hydroxyalkyl)-3-nitrosoureas, 1-(2-hydroxyethyl)-3-(2-chloroethyl)-3-nitrosourea yielded more cures (90%) than did BCNU (cure rate, 70%) and was also superior to the other substances. Against preterminal ip implanted and late intracerebrally implanted L5222, the hydroxyethyl compound was significantly superior to BCNU.

Keywords

This publication has 2 references indexed in Scilit:

Development of meningeal leukemia in rats by intracerebral or intrameningeal inoculation of the acute transplantable leukemia L 5222
Zeitschrift für Krebsforschung und Klinische Onkologie, 1976
A Simple Method to Inject Drugs Intracerebrally
Pharmacology, 1964