title: Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors.
abstract: In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine via GK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity.
authors.affiliation: Innovative Drug Library Research Center, Dongguk University, Seoul, 100-715, Republic of Korea. ydgong@dongguk.edu.
authors.forename: Nayeon
authors.initials: N
authors.lastname: Kim
authors.forename: Se Hun
authors.initials: SH
authors.lastname: Kwak
authors.forename: Seon-Hyeong
authors.initials: SH
authors.lastname: Lee
authors.forename: Vinayak
authors.initials: V
authors.lastname: Juvekar
authors.forename: Byung-Il
authors.initials: BI
authors.lastname: Lee
authors.forename: Hee-Chul
authors.initials: HC
authors.lastname: Ahn
authors.forename: Soo-Youl
authors.initials: SY
authors.lastname: Kim
authors.forename: Young-Dae
authors.initials: YD
authors.lastname: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D019204:GTP-Binding Proteins / Q000037:antagonists & inhibitors*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D062105:Molecular Docking Simulation; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011503:Transglutaminases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011719:Pyrazines; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011503:Transglutaminases; D019204:GTP-Binding Proteins