Tag: M.W=350-400

Zheng, Lin published the artcileThe calcimimetic agent cinacalcet inhibits hepatocellular carcinoma via YAP/TAZ suppression, Safety of 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, the publication is Pharmazie (2021), 76(10), 511-514, database is CAplus and MEDLINE.

The lack of effective strategies remains a pivotal challenge for hepatocellular carcinoma (HCC) treatment. YAP/ TAZ is a promising target for effective drugs against HCC. In this study, we profiled the regulatory effect of 98 drugs on transcriptional activity of YAP/TAZ and identified the calcimimetic agent cinacalcet as a potent YAP inhibitor. Cinacalcet inhibited YAP expression in HCC models at both transcriptional and protein levels, and ultimately arrested cell proliferation of HCC. Overexpression of YAP weakened the anticancer efficacy of cinacalcet, indicating that YAP was responsible for the antineoplastic activity of cinacalcet. Collectively, this study suggested cinacalcet as a feasible anticancer drug for HCC via its inhibition on YAP/TAZ.

Pharmazie published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C10H10O2, Safety of 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

Di Rocco, Daniel A. published the artcileLate-stage functionalization of biologically active heterocycles through photoredox catalysis, Quality Control of 375815-87-5, the publication is Angewandte Chemie, International Edition (2014), 53(19), 4802-4806, database is CAplus and MEDLINE.

The direct C-H functionalization of heterocycles has become an increasingly valuable tool in modern drug discovery. However, the introduction of small alkyl groups, such as Me, by this method has not been realized in the context of complex mol. synthesis since existing methods rely on the use of strong oxidants and elevated temperatures to generate the requisite radical species. Herein, the authors report the use of stable organic peroxides activated by visible-light photoredox catalysis to achieve the direct methyl-, ethyl-, and cyclopropylation of a variety of biol. active heterocycles. The simple protocol, mild reaction conditions, and unique tolerability of this method make it an important tool for drug discovery.

Angewandte Chemie, International Edition published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Quality Control of 375815-87-5.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider