Xu, Shengtao published the artcileA Novel Potent Anticancer Compound Optimized from a Natural Oridonin Scaffold Induces Apoptosis and Cell Cycle Arrest through the Mitochondrial Pathway, Application In Synthesis of 6313-54-8, the publication is Journal of Medicinal Chemistry (2017), 60(4), 1449-1468, database is CAplus and MEDLINE.
The cytotoxicity of the natural ent-kaurene diterpenoid, oridonin, has been extensively studied. However, the application of oridonin for cancer therapy was hampered primarily by its moderate potency. In this study, a series of oridonin A-ring modified analogs, and their derivatives bearing various substituents on 14-OH position, were designed, synthesized and evaluated for anticancer efficacy. Some of the derivatives were significantly more potent than oridonin against both drug-sensitive and drug-resistant cancer cells. The most potent compound, I, was 200-fold more efficacious than oridonin in MCF-7 cancer cells. Furthermore, I induced apoptosis and cell cycle arrest at the G2/M phase. A decrease in mitochondrial membrane potential and increased Bax/Bcl-2 ratio, accompanied by activated caspase-3 cleavage, were observed in MCF-7 cells after treatment with I, suggesting that the mitochondrial pathway was involved in the I-mediated apoptosis. Moreover, I significantly inhibited tumor growth in mouse xenograft models and had no observable toxic effect.
Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C5H7FO2, Application In Synthesis of 6313-54-8.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics