Identification of Lead Compounds as Inhibitors of STAT3: Design, Synthesis and Bioactivity

STAT3 belongs to the signal transducers and activators of transcription (STAT) family. It has been demonstrated that STAT3 is constitutively activated in many tumors, playing a role in carcinogenesis and tumor progression. For this reason, it has being considered a potential target for cancer therapy. In this context, we have designed, synthesized and evaluated 1,​4-​dimethyl-​carbazole derivs., targeting the STAT3 protein. Moreover, MTT assay performed on A375 and HeLa, showed significant antiproliferative activity of some of synthesized compds. (3-​5)​. The same compds. (3-​5) considerably reduced STAT3 expression, as demonstrated by Western blot anal. Our multidisciplinary approach shows that 1,​4-​dimethyl-​carbazoles are potential building blocks to develop more affinity ligands of STAT3.