1038352-61-2Relevant academic research and scientific papers
TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAN (TEAD) TRANSCRIPTION FACTOR INHIBITORS AND USES THEREOF
-
Paragraph 00301; 00399; 00402-00403; 00488; 00491-00492, (2021/07/02)
Provided herein are compounds of (I-A), (I-B), or (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are methods, uses,
One-pot propagation of (Hetero)Arylamines: Modular synthesis of diverse Amino-di(hetero)arylamines
Liang, Xueting,Xu, Liang,Li, Cuihua,Jia, Xin,Wei, Yu
, p. 721 - 731 (2019/01/08)
Formal propagation of (hetero)arylamine is achieved via a one-pot Buchwald–Hartwig C–N cross-coupling and nitro reduction sequence, enabling a rapid modular synthesis of diverse amino-di(hetero)arylamines from (hetero)arylamines and halogenated nitrobenzenes. Various functionalized aromatic amines with different electronic and steric environments can be efficiently prolongated to formally incorporate another arylamino fragments. This approach has been successfully applied in the synthesis of more than forty amino-di(hetero)arylamines. The applicability of this method has also been demonstrated in the synthesis of oligoanilines and the tyrosine-kinase inhibitor Imatinib.
Identification of less lipophilic riminophenazine derivatives for the treatment of drug-resistant tuberculosis
Zhang, Dongfeng,Liu, Kai,Liu, Binna,Wang, Jingbin,Zhang, Gang,Zhang, Hao,Liu, Yang,Hou, Yanyan,Gong, Ningbo,Lv, Yang,Li, Chun,Yin, Dali,Huang, Haihong,Lu, Yu,Wang, Bin,Zheng, Meiqin,Fu, Lei,Cooper, Christopher B.,Upton, Anna M.,Ma, Zhenkun
, p. 8409 - 8417,9 (2020/09/15)
Clofazimine (CFZ), a member of the riminophenazine class, has been studied in clinical trials for the treatment of multidrug-resistant tuberculosis (MDR-TB). CFZ has several side effects which can be attributed to its extremely high lipophilicity. A series of novel riminophenazine analogues bearing a C-2 pyridyl substituent was designed and synthesized with the goal of maintaining potent activity against Mycobacterium tuberculosis (M. tuberculosis) while improving upon its safety profile by lowering the lipophilicity. All compounds were evaluated for their in vitro activity and cytotoxicity. The results demonstrated that many new compounds had potent activity against M. tuberculosis with MICs of less than 0.03 μg/mL and low cytotoxicity with IC50 values greater than 64 μg/mL. Some compounds were tested for in vivo efficacy against MDR-TB in an experimental mouse infection model. Two compounds demonstrated equivalent or better efficacy than CFZ in this model with significantly reduced skin discoloration potential.
