title: Identification of Lead Compounds as Inhibitors of STAT3: Design, Synthesis and Bioactivity.
abstract: 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 derivatives, targeting the STAT3 protein. Moreover, MTT assay performed on A375 and HeLa, showed significant antiproliferative activity of some of synthesized compounds (3-5). The same compounds (3-5) considerably reduced STAT3 expression, as demonstrated by Western blot analysis. Our multidisciplinary approach shows that 1,4-dimethyl-carbazoles are potential building blocks to develop more affinity ligands of STAT3.
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax).
authors.forename: Antonio
authors.initials: A
authors.lastname: Botta
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax).
authors.forename: Esther
authors.initials: E
authors.lastname: Sirignano
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax).
authors.forename: Ada
authors.initials: A
authors.lastname: Popolo
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax). saturnino@unisa.it.
authors.forename: Carmela
authors.initials: C
authors.lastname: Saturnino
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax).
authors.forename: Stefania
authors.initials: S
authors.lastname: Terracciano
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax).
authors.forename: Antonio
authors.initials: A
authors.lastname: Foglia
authors.affiliation: Dipartimento di Chimica e Biologia, Università degli Studi di Salerno Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy.
authors.forename: Maria Stefania
authors.initials: MS
authors.lastname: Sinicropi
authors.affiliation: Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, 87036 Arcavacata di Rende, Cosenza, Italy.
authors.forename: Pasquale
authors.initials: P
authors.lastname: Longo
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy phone/fax: +39 089969176 (S. D. M.); +39 089969769 (C. S.); +39 089969602 (fax). sdimicco@unisa.it.
authors.forename: Simone
authors.initials: S
authors.lastname: Di Micco
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D007854:Lead / Q000737:chemistry / Q000494:pharmacology; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D009369:Neoplasms / Q000737:chemistry / Q000188:drug therapy / Q000378:metabolism; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles; D009363:Neoplasm Proteins; D050796:STAT3 Transcription Factor; C494086:STAT3 protein, human; D007854:Lead
keywords: 1,4-dimethyl-carbazoles; Antitumor compound; Molecular docking; STAT3; STAT3 inhibitor