1055995-87-3Relevant articles and documents
Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors
Xue, Ding,Xu, Yibin,Kyani, Armita,Roy, Joyeeta,Dai, Lipeng,Sun, Duxin,Neamati, Nouri
, p. 343 - 368 (2022/01/20)
Inhibition of oxidative phosphorylation (OXPHOS) is a promising therapeutic strategy for select cancers that are dependent on aerobic metabolism. Here, we report the discovery, optimization, and structure-activity relationship (SAR) study of a series of n
MITOCHONDRIAL TARGETING COMPOUNDS FOR THE TREATMENT OF ASSOCIATED DISEASES
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Page/Page column 63; 76, (2021/12/08)
Mitochondrial targeting compounds for the treatment of cancer and other disorders associated with mitochondrial function, including diabetes, autoimmune diseases, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases and their preparation. The present invention is also directed to the pharmaceutical compositions and treatment methods, prodrugs based on those compounds and the use thereof.
Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening
Zhang, Rukang,Wang, Jiang,Zhao, Liang,Liu, Shien,Du, Daohai,Ding, Hong,Chen, Shijie,Yue, Liyan,Liu, Yu-Chih,Zhang, Chenhua,Liu, Hong,Luo, Cheng
, p. 867 - 876 (2018/08/28)
The histone acetyltransferases (HATs) in mammals include GCN5 N-acetyltransferases, the MOZ, YBF2, SAS2, and TIP60 proteins, and the orphan HATs. The males absent on the first (MOF) is mainly related to acetylation of histone H4 Lys16 and has influence on downstream genes expression. However, the only inhibitor MG149 presented low activity against MOF. Besides, there was no high throughput screening platform on MOF, which limited the inhibitor discovery and functional study. In our study, we set up a high throughput screening platform based on amplified luminescent proximity homogeneous assay (ALPHA), which led us to a moderate inhibitor DC_M01. By chemical modification, we found DC_M01_7, which was the analog of DC_M01 with an IC50 value of 6 μM. DC_M01_7 significantly inhibited HCT116 cells proliferation and could also inhibit histone 4 lysine 16 acetylation in HCT116 cells. To sum up, our work will probably assist the further development of more potent MOF inhibitors and the functional study of hMOF.
ARYL SULFONAMIDES USEFUL FOR MODULATION OF THE PROGESTERONE RECEPTOR
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Page/Page column 22, (2008/12/08)
In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; trea