33948-19-5Relevant articles and documents
Synthesis and Biological Evaluation of Celastrol Derivatives with Improved Cytotoxic Selectivity and Antitumor Activities
Feng, Jia-Hao,He, Qi-Wei,Hou, Ji-Qin,Hu, Xiao-Long,Long, Huan,Wang, Bao-Lin,Wang, Hao,Wang, Quan,Wang, Rong,Ye, Wen-Cai,Zhang, Li-Xin,Zhang, Xiao-Qi
, p. 1954 - 1966 (2021/07/20)
Cdc37 associates kinase clients to Hsp90 and promotes the development of cancers. Celastrol, a natural friedelane triterpenoid, can disrupt the Hsp90-Cdc37 interaction to provide antitumor effects. In this study, 31 new celastrol derivatives, 2a - 2d , 3a - 3g , and 4a - 4t , were designed and synthesized, and their Hsp90-Cdc37 disruption activities and antiproliferative activities against cancer cells were evaluated. Among these compounds, 4f , with the highest tumor cell selectivity (15.4-fold), potent Hsp90-Cdc37 disruption activity (IC50= 1.9 μM), and antiproliferative activity against MDA-MB-231 cells (IC50= 0.2 μM), was selected as the lead compound. Further studies demonstrated 4f has strong antitumor activities both in vitro and in vivo through disrupting the Hsp90-Cdc37 interaction and inhibiting angiogenesis. In addition, 4f exhibited less toxicity than celastrol and showed a good pharmacokinetics profile in vivo. These findings suggest that 4f may be a promising candidate for development of new cancer therapies.
Synthetic method of oxcarbazepine
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Paragraph 0013, (2017/08/31)
The invention relates to a synthetic method of oxcarbazepine. According to the method, the oxcarbazepine is prepared from iminodibenzyl as a raw material through formyl chlorination, dihalogenated dehydrohalogenation, ammonification and hydrolyzation; a product obtained after formyl chlorination is iminodibenzyl-5-carbonyl chloride, wherein the dihalogenated dehydrohalogenation process specifically comprises the step that the iminodibenzyl-5-carbonyl chloride and a halogenating reagent react for 3-6 h at the temperature ranging from 80 DEG C to the reflux temperature in the presence of an organic solvent and an initiating agent to obtain a disubstituted halogenated product, then the disubstituted halogenated product reacts for 8-16 h at the reflux temperature to be subjected to dehydrohalogenation to obtain 10-halo-5H-dibenzoazepine-5-formyl chloride. The method has the advantages that starting materials are low in price and easy to obtain; the processing step is short; the yield is high; and the cost is low.
Piperidine derivatives
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, (2008/06/13)
Piperidine derivatives of formula STR1 wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R 1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R 2 is alkyl or phenyl; and R 3 is phenyl optionally substituted, or R 3 is STR2 wherein Z represents a 5- or 6-membered heterocyclic ring; or R 2 and R 3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.