With our interest in （S）-3-aminopyrrolidine derivatives,we further screened inhibition activities of three hit compounds on many other kinases with the results demonstrating that this series of compounds shows bette...With our interest in （S）-3-aminopyrrolidine derivatives,we further screened inhibition activities of three hit compounds on many other kinases with the results demonstrating that this series of compounds shows better anticancer activities,which might result from the main block of PI3K/Akt signaling pathway and the inhibition of Abelson murine leukemia viral oncogene homolog（ABL） kinase,as well as some epidermal growth factors.Further structure modification demonstrates that benzylsulfonyl group is the necessary functional group contributing to the biological activity that will be helpful to guiding us to optimize these （S）-3-aminopyrrolidine derivatives.展开更多
Sixteen resveratrol analogs（stilbene derivatives） including resveratrol were synthesized, in which hy- droxystilbenes, naturally occurring polyphenols, showed protective effects against reactive oxygen and nitrogen ...Sixteen resveratrol analogs（stilbene derivatives） including resveratrol were synthesized, in which hy- droxystilbenes, naturally occurring polyphenols, showed protective effects against reactive oxygen and nitrogen spe- cies（ROS/RNS） and hexahydroxystilbene（16） displayed the strongest activities against NO and l,l-diphenyl- 2-picrylhydrazyl（DPPH） with IC5o values of 7.8 and 5.7 μmol/L, respectively.展开更多
文摘With our interest in （S）-3-aminopyrrolidine derivatives,we further screened inhibition activities of three hit compounds on many other kinases with the results demonstrating that this series of compounds shows better anticancer activities,which might result from the main block of PI3K/Akt signaling pathway and the inhibition of Abelson murine leukemia viral oncogene homolog（ABL） kinase,as well as some epidermal growth factors.Further structure modification demonstrates that benzylsulfonyl group is the necessary functional group contributing to the biological activity that will be helpful to guiding us to optimize these （S）-3-aminopyrrolidine derivatives.
基金Supported by the Shenzhen Science and Technology Program, China（No.JCYJ20120830153011458）, the Project of the Edu- cational Commission of Guangdong Province of China（No.2013KJCX0164） and the Natural Science Foundation of Shenzhen Universitiy, China（No.00036159）.
文摘Sixteen resveratrol analogs（stilbene derivatives） including resveratrol were synthesized, in which hy- droxystilbenes, naturally occurring polyphenols, showed protective effects against reactive oxygen and nitrogen spe- cies（ROS/RNS） and hexahydroxystilbene（16） displayed the strongest activities against NO and l,l-diphenyl- 2-picrylhydrazyl（DPPH） with IC5o values of 7.8 and 5.7 μmol/L, respectively.
