| abstract |
Referring to a compound of formula (II) wherein R2 is alkyl, cycloalkylalkyl, aralkyl, among others; X6 is C-H or N; X5 is C-R5 or N; R5 is H, halogen, OH, CN, among others; R6 is H, halogen, -OH, -CN, among others; RA is (B); X2 is N or C-R12; R12 is H, halogen, alkyl, alkoxy; R13 is -Y-Z; Y is a bond, -CH2, among others; Z is SO2R21; -N (R22) SO2R21, among others; X3 is N or C-R14; R14 is H, halogen, CN, among others; X4 is N or CR15; R15 is H, halogen, alkyl, among others; R16 is H, halogen, among others; R21 is alkyl, cycloalkylalkyl, aryl, among others; R22 is H, alkyl, cycloalkyl, aryl, among others. These compounds are heterocycle derivatives that have activity on epigenetic regulation by inhibiting bromodomain-mediated recognition of regions of acetyl-lysine proteins such as histones; being useful in the treatment of cancer and neoplastic diseases such as Burkitt's lymphoma, prostate cancer, melanoma, among others. |