Microorganism of genus chrysosporium for use in preparing farnesyl transferase inhibitors
AssigneeRhone-Poulenc Rorer S.A.
InventorsJean Leboul, Didier Van der Pyl, Jean-Jacques Debernard
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Abstract
A Chrysosporium strain No. CBS 123.95, mutants and derivatives thereof, and a method for preparing non-peptide compounds using said strain, are disclosed. Novel compounds of general formula (I), pharmaceutical compositions containing same, and the use of said compounds in anticancer treatments, are also disclosed.
Claims12
A compound of the general formula I ##STR6## in which:
- R.sub.1 represents a C.sub.1 to C.sub.5 alkoxy group, an aldehyde group, a carboxyl group, a C.sub.1 to C.sub.5 alkyl ester or a (C.sub.1 to C.sub.5 alkyl)hydroxyl group,
- R.sub.2 represents a hydrogen atom or a C.sub.1 to C.sub.4, linear or branched, lower alkyl group, and
- R.sub.3 represents a C.sub.1 to C.sub.4 alkyl group, a hydroxyl group or a C.sub.1 to C.sub.4 alkoxy group,
- or salt thereof.
A method of inhibiting farnesyl transferase activity comprising combining a sufficient quantity of the compound of formula I to effect inhibition of farnesyl transferase activity, with a composition containing farnesyl transferase.
A compound of the general formula II:
- ##STR7## in which:
- R.sub.2 and R.sub.4 represent, independently of each other, a hydrogen atom or a C.sub.1 to C.sub.4, linear or branched, lower alkyl group, and
- R.sub.5 represents a hydrogen atom, a C.sub.1 to C.sub.5 alkyl group, where appropriate substituted with a group chosen from the hydroxyl or phenyl groups, optionally substituted with one or more methyl, methoxy, hydroxyl or halogen groups, or salt thereof.
A compound of formula ##STR8## or salt thereof.
Chrysosporium strain No. CBS 123.95 or mutant thereof or derivative thereof.
Dependencies are inferred from the claim text.