Inventors:
Nigel H. Greig - Washington DC
Daniel J. Sweeney - Indianapolis IN
Stanley I. Rapoport - Washington DC
Assignee:
The United States of America as represented by the Department of Health
and Human Services - Washington DC
International Classification:
A61K 31245, C07C10164
Abstract:
Tertiary butyl esters of anticancer drugs are provided which have the following formula: ##STR1## wherein R. sub. 1 and R. sub. 2 are the same or different and are selected from the group consisting of H, F, Cl, Br, and I and R. sub. 2 can also be NH. sub. 2 ;
R. sub. 3, R. sub. 4, and R. sub. 5 are the same or different and are selected from the group consisting of H, F, Cl, Br, I, and C. sub. 1 -C. sub. 3 alkyl; wherein alkyl may be substituted with F, Cl, Br, or I, with the proviso that at least two of R. sub. 3, R. sub. 4, and R. sub. 5 are alkyl or substituted alkyl; and
n=0-4.
The compounds of the present invention can be used in treating cancer by significantly increasing the brain levels of the drugs of the invention and their active metabolites.