Biological Evaluation and Structure Modification of (S)-3-Aminopyrrolidine Derivatives

doi:10.1007/s40242-014-3174-3

Chemical Research in Chinese Universities ›› 2014, Vol. 30 ›› Issue (1): 91-97.doi: 10.1007/s40242-014-3174-3

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Biological Evaluation and Structure Modification of (S)-3-Aminopyrrolidine Derivatives

XIN Tian^1,2,3, ZHANG Cunlong^2,3, TAN Chunyan^2,3, JIANG Yuyang^1,2,3,4

1. Department of Chemistry, Tsinghua University, Beijing 100084, P. R. China;
2. State Key Laboratory Breeding Base-Shenzhen Key Laboratory of Chemical Biology, Tsinghua University, Shenzhen 518055, P. R. China;
3. Shenzhen Anti-tumor Drug Development Engineering Laboratory, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, P. R. China;
4. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, P. R. China

Received:2013-04-17 Revised:2013-05-15 Online:2014-02-01 Published:2013-06-13
Contact: TAN Chunyan,E-mail:jiangyy@sz.tsinghua.edu.cn; JIANG Yuyang,E-mail:tancy@sz.tsinghua.edu.cn E-mail:jiangyy@sz.tsinghua.edu.cn; tancy@sz.tsinghua.edu.cn
Supported by:
Supported by the National Science and Technology Major Special Project for New Drug Research and Design of China (No.2012ZX09506001-010) and the National Basic Research Program of China(No.2012CB722605).

Abstract

Abstract:

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.

Key words: (S)-3-Aminopyrrolidine, Biological evaluation, Structure modification

XIN Tian, ZHANG Cunlong, TAN Chunyan, JIANG Yuyang. Biological Evaluation and Structure Modification of (S)-3-Aminopyrrolidine Derivatives[J]. Chemical Research in Chinese Universities, 2014, 30(1): 91-97.

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Biological Evaluation and Structure Modification of (S)-3-Aminopyrrolidine Derivatives

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