Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors

• Published in: European journal of medicinal chemistry Vol. 174; pp. 236 - 251
• Main Authors: Cai, Guiping, Yu, Wenying, Song, Dongmei, Zhang, Wenda, Guo, Jianpeng, Zhu, Jiawen, Ren, Yuhao, Kong, Lingyi
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 15.07.2019; Elsevier
• Subjects: Antitumor activity; Benzo[b]thiophene 1, 1-Dioxide; Chemistry, Medicinal; Life Sciences & Biomedicine; Mitochondrial apoptosis pathway; N, N-Diethyl-7-aminocoumarin fluorophore; Pharmacology & Pharmacy; Science & Technology; Ser727 phosphorylation; STAT3; PBS; rt; Src; DMSO; STAT3; Ser727 phosphorylation; N, N-Diethyl-7-aminocoumarin fluorophore; MTT; Mitochondrial apoptosis pathway; STAT; FBS; ROS; Antitumor activity; PI; Benzo[b]thiophene 1, 1-Dioxide; TMS; JAK2; SH2; GAPDH; JC-1; Erk; ACTIVATION; DESIGN; TRANSCRIPTION; SERINE PHOSPHORYLATION; CANCER; SMALL-MOLECULE INHIBITOR; TYROSINE; BIOLOGICAL EVALUATION; DERIVATIVES; SIGNAL TRANSDUCER

STAT3 has been extensively studied as a potential antitumor target. Though studies on regulating STAT3 mainly focus on the inhibition of STAT3 phosphorylation at Tyr705 residue, the phosphorylation at Ser727 residue of STAT3 protein is also closely associated with the mitochondrial import of STAT3 p...