5680-80-8Relevant articles and documents
Synthesis and Biological Evaluation of a Series of Novel Celastrol Derivatives with Amino Acid Chain
Pang, Chaohai,Luo, Jinhui,Liu, Chunhua,Wu, Xuejin,Wang, Dingyong
, (2018/05/04)
The synthesis of celastrol analogues containing amino acid ester at the C(29) position and their evaluation for cytotoxic activities in?vitro were reported. The MTT test showed that a set of derivatives with lower IC50 values than that of the positive control group cisplatin and the parent compound celastrol, which exhibited greater antiproliferative activities. The most potent title compounds 2a and 2e exhibited cytotoxic activities in?vitro against HeLa and A549 cell lines with IC50 values of 0.371 and 0.237?μm, 0.235 and 0.109?μm, respectively. The apoptosis assay demonstrated that 2a and 2e can induces of A549 cell apoptosis in low concentrations. These results showed that 2a and 2e may be promising for further research as antitumor agents.
DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
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Paragraph 00319; 00320, (2014/10/04)
Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
PYRIMIDINE NUCLEOSIDE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF FOR PREPARING ANTI-TUMOR AND ANTI-VIRUS MEDICAMENTS
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Paragraph 0068, (2013/11/19)
The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.