Abstract: A GRK2 protein inhibitor compound of Formula I wherein X is an atom selected from carbon and nitrogen, and R1 is selected from the groups methyl carboxylate and 1,3,4-oxadiazol-2-yl and wherein the compound is selected from methyl 4-(naphthalene-2-amido)benzoate and N-[4-(1,3,4-oxadiazol-2-yl)phenyl]quinoline-3-carboxamide. Also disclosed are pharmaceutical compositions comprising at least a compound of Formula I.

Abstract: A new compound of formula A for the treatment of aggressive and/or resistant tumors expressing acyl-CoA synthetase 4 (ACSL4) and/or depending on steroids action. More particularly, the compound of the present invention inhibits tumor growth in ACSL4-expressing breast and prostate cancers, inhibits steroid synthesis and sensitizes cells towards chemotherapeutic and hormone therapy agents. Pharmaceutical compositions comprising the ACSL4-inhibitory compound of the invention, pharmaceutical combinations thereof with other anticancer agents and use in therapy.

Abstract: Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumors, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.

Abstract: Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumours, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.

Abstract: The present invention relates to a compound having inhibitory activity on a Rho-GTPase cell protein, the compound having the formula I (Formula I) wherein A is selected from N and N—H, R1 is selected from H and NHR3, R2 is selected from NHR4, OR4, O and halogen, R3 is selected from H and —COR5, R4 is selected from H, a C1-C6 alkyl and a substituted or unsubstituted phenyl, R5 is selected from a C1-C12 alkyl and a substituted or unsubstituted phenyl, R6 is selected from H, —COR5, —CO2R5, —PR7R8 and —PR7R8OPR7R8R8R7, R7 is selected from O and S, R8 is selected from H, OR4 and OSATE (—OCH2CH2SCOR5), and wherein each represents a single bond or a double bond, provided that when one of them is a double bond the other one is a single bond, and pharmaceutically acceptable salts and derivatives thereof. In particular, the compounds of the invention may be used as antitumor agents the action of which interfere with the signaling pathways normally involved in tumor development processes.