专利号:US-10471054-B2 优先权日:2016-06-15 标 题 :CDK1 inhibitors of acetyl chrysin mannich base derivatives, synthesis and use thereof 发明人:ZHANG FAN; ZHANG SHIXUAN; JU XIULAN 权利人:ZHANG FAN 摘要:Provided is a series of acetyl Chrysin Mannich base derivatives with the structures illustrated in the following scheme: wherein R 1 is acetyl and R 2 is cycloalkylamine-methyl, or R 2 is acetyl and R 1 is cycloalkylamine-methyl. Such derivatives are cyclin-dependent protein kinases 1 (CDK1) selective inhibitors. Base on the levels of .O 2 − and Fe ++ are higher 5-15 times in cancer cells than in normal cells, the action mechanism of such derivatives by regulating intracellular reactive oxygen species (ROS) is activating mitochondria apoptosis pathway without the death receptor pathway, thus selectively inducing apoptosis of cancer cells and protecting normal cells. Inside, CH-j has a good druggability for the selectivity of solid cancers. Moreover, CH-f has also a good druggability for the systemic cancers.
专利号:RU-2026296-C1 优先权日:1988-06-20 标题 :Method of synthesis of nitrogen-containing heterocyclic compounds or their pharmaceutically acceptable salts
专利号:US-9868695-B2 优先权日:2014-10-14 标 题:10-substituted colchicinoids as potent anticancer agents 发明人:VISHWAKARMA RAM A; BHARATE SANDIP B; KUMAR AJAY; SINGH BALJINDER; KUMAR ASHOK; BHUSHAN SHASHI; HAMID ABID; JOSHI PRASHANT; GURU SANTOSH K; KUMAR SURESH; HUSSAIN AASHIQ; QAZI ASIF K; BHARATE SONALI S; SHARMA PARDUMAN; SAXENA AJIT K; MONDHE DILIP M; MAHAJAN GIRISH; WANI ZAHOOR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to the compounds of formula I wherein R is as herein described. The present invention particularly relates to synthesis and antiproliferative activity of 10-substituted colchicinoids. Compounds of the invention can be used for prevention or in the treatment of cancer disease.
专利号:US-2019216792-A1 优先权日:2016-06-15 标题:Cdk1 inhibitors of acetyl chrysin mannich base derivatives, synthesis and use thereof