COMPOUNDS FOR USE IN STABILISING p53 MUTANTS

摘要

Provided are compounds for use in a method of treatment of a subject who has a lesion or a tumour in which p53 carries a Y220C mutation, in which the compound is selected from compounds of the following formula (I), and pharmaceutically acceptable salts, hydrates, and solvates thereof: (I) R: where A is CR4 or N; -R-1 is selected from -OH, -OMe, -NH2, -SH, -F and -CF3; -R2 is selected from -CI, -Br, -I, and ethynyl (-C=CH); -R3 is selected from -I, -Br, -CI, ethynyl (-C=CH), -R35, -H, -OMe, and -N02; wherein -R3S is selected from: and -R5 is selected from -COOH and: 8A formula Ilia formula 1Mb formula 111 o 3 where -R6, -R7A, - R7B, -Rs, and -R8A are as defined in the specification. Compounds of formula (I) are also provided, as is their use in methods of treatment, and methods for their preparation.