Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents
Jiali Ji
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorFarrukh Sajjad
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorQun You
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorDong Xing
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorHui Fan
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorAlavala G. K. Reddy
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China
Search for more papers by this authorCorresponding Author
Wenhao Hu
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China
Correspondence Wenhao Hu, School of Pharmaceutical Sciences, Sun Yat-sen University, 510006 Guangzhou, China.
Email: [email protected]
Suzhen Dong, Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Rd., 200062 Shanghai, China.
Email: [email protected]
Search for more papers by this authorCorresponding Author
Suzhen Dong
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Key Laboratory of Brain Functional Genomics, Ministry of Education, East China Normal University, Shanghai, China
Correspondence Wenhao Hu, School of Pharmaceutical Sciences, Sun Yat-sen University, 510006 Guangzhou, China.
Email: [email protected]
Suzhen Dong, Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Rd., 200062 Shanghai, China.
Email: [email protected]
Search for more papers by this authorJiali Ji
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorFarrukh Sajjad
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorQun You
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorDong Xing
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorHui Fan
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Search for more papers by this authorAlavala G. K. Reddy
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China
Search for more papers by this authorCorresponding Author
Wenhao Hu
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China
Correspondence Wenhao Hu, School of Pharmaceutical Sciences, Sun Yat-sen University, 510006 Guangzhou, China.
Email: [email protected]
Suzhen Dong, Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Rd., 200062 Shanghai, China.
Email: [email protected]
Search for more papers by this authorCorresponding Author
Suzhen Dong
Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China
Key Laboratory of Brain Functional Genomics, Ministry of Education, East China Normal University, Shanghai, China
Correspondence Wenhao Hu, School of Pharmaceutical Sciences, Sun Yat-sen University, 510006 Guangzhou, China.
Email: [email protected]
Suzhen Dong, Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Rd., 200062 Shanghai, China.
Email: [email protected]
Search for more papers by this authorJiali Ji and Farrukh Sajjad contributed equally to this study.
Abstract
A series of polysubstituted pyrrolidines obtained via ruthenium-catalyzed cascade cyclization of diazo pyruvates and anilines as well as their corresponding pyrrole analogs obtained via dehydration were evaluated for their antiproliferation activities. Pyrrolidines 3h and 3k showed good proliferation inhibitory effects toward 10 cancer cell lines with IC50 values ranging from 2.9 to 16 μM. Furthermore, pyrrolidine 3k induced cell cycle arrest at the G0/G1 phase and time- and dose-dependent cellular apoptosis in both HCT116 and HL60 cells, suggesting that this type of pyrrolidine structure might be a good candidate for future anticancer therapies.
CONFLICTS OF INTERESTS
The authors declare that there are no conflicts of interests.
Supporting Information
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