43034-86-2Relevant academic research and scientific papers
TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAIN (TEAD) TRANSCRIPTION FACTOR INHIBITORS AND USES THEREOF
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, (2020/05/21)
Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, compositions, and mixtures thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.
Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B
Liu, Moyi,Xu, Qiaoling,Guo, Su,Zuo, Ruixi,Hong, Yue,Luo, Yong,Li, Yingxiu,Gong, Ping,Liu, Yajing
, p. 2621 - 2631 (2018/04/30)
The hepatitis C virus (HCV) NS5B polymerase is an attractive target for the development of novel and selective inhibitors of HCV replication. In this paper, the design, synthesis, and preliminary SAR studies of novel inhibitors of HCV NS5B polymerase based on the structure of tegobuvir have been described. The efforts to optimize the antiviral potency and reduce the treatment side effects with respect to genotype 1b resulted in the discovery of compound 3, which exhibited an EC50 of 1.163 nM and a CC50 >200 nM in a cell-based HCV replicon system assay. Additionally, testing for inhibition of the hERG channel showed a marked improvement over tegobuvir and the pharmacokinetic properties of compound 3 indicated that it was worthy of further investigation as a non-nucleoside inhibitor of HCV NS5B polymerase.
Design, synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors
Zhang, Aigui,Zhou, Jingya,Tao, Ke,Hou, Taiping,Jin, Hong
, p. 3042 - 3045 (2018/08/11)
Sixteen novel pyrazole carboxamides with diarylamines scaffold were designed, synthesized and characterized in detail via 1H NMR, 13C NMR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good ant
ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
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Page/Page column 142, (2008/12/06)
The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Synthesis and Characterization of Water-Soluble and Photolabile 10-Arylisoalloxazines: Tools for Studying the Mechanism of Action of Flavin-Type Antimalarials
Kirsch, Peer,Schoenleben-Janas, Annette,Schirmer, R. Heiner
, p. 1275 - 1282 (2007/10/02)
Isoalloxazine derivatives such as 1a-d are promising antimalarial agents which act as inhibitors of the antioxidant enzyme glutathione reductase and possibly of other proteins.The molecular mechanism of the pharmacological effects has not been studied in detail because compounds 1a-d are poorly soluble in aqueous solutions of physiological pH.In the present study we introduce two new types of isoalloxazine derivatives with improved solubility properties.The 10-aryl-3-carboxymethylisoalloxazines 2a-d, and the isomeric 3-methyl-10-(N-methylpyridiniumyl)isoalloxazine salts 3 and 4.In addition, for the purpose of photoaffinity labeling experiments, the 10-aryl-8-azido-3-methylisoalloxazine 5 was designed.The syntheses and characterizations of these new flavins as well as an alternative synthetic approach to the known antimalarials 1a-d are described. - Keywords: Flavins/Isoalloxazines/Arylisoalloxazines/Malaria/Antimalarials/Glutathione reductase inhibitors/Photoaffinity labels
