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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Zhou, Rui Wang, Biao Zhao, Qian Huang, Wei Peng, Cheng Peng, Fu Leng, Hai-jun Zingales, Sarah He, Gu Han, Bo |
| Description | Author Affiliation: Leng HJ ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China).); Peng F ( School of Chinese Medicine, University of Hong Kong, Hong Kong (P.R. China).); Zingales S ( Department of Chemistry, Armstrong State University, Savannah, GA (USA).); Huang W ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China).); Wang B ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China).); Zhao Q ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China).); Zhou R ( State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041 (P.R. China).); He G ( State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041 (P.R. China). hegu@scu.edu.cn.); Peng C ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China). pengcheng@cdutcm.edu.cn.); Han B ( State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137 (P.R. China). hanbo@cdutm.edu.cn.) |
| Abstract | The highly enantioselective preparation of pharmacologically interesting hexahydropyridazine derivatives based on a multicomponent cascade reaction is described. This one-pot approach utilizes an organocatalytic Michael reaction followed by intermolecular α-amination and intramolecular hemiaminalization to yield a chiral pyridazine backbone with contiguous stereogenic centers and multiple functional groups in good yield and with high stereoselectivity. Compounds synthesized by this method potently inhibited proliferation of MCF-7 breast cancer cells. Mechanistic studies suggest that compound 5 c exerts these anticancer effects by inducing apoptosis through extracellular signal related kinase (ERK)- and poly(adenosine diphosphate ribose) polymerase (PARP)-regulated pathways, as well as mitochondrial pathways. |
| ISSN | 09476539 |
| e-ISSN | 15213765 |
| Journal | Chemistry - A European Journal |
| Issue Number | 50 |
| Volume Number | 21 |
| Language | English |
| Publisher | Wiley-VCH;ChemPubSoc Europe |
| Publisher Date | 2015-12-07 |
| Publisher Place | Germany |
| Access Restriction | Open |
| Subject Keyword | Apoptosis Drug Effects Breast Neoplasms Drug Therapy Cell Proliferation Poly(ADP-ribose) Polymerase Inhibitors Chemistry Pharmacology Pyridines Chemical Synthesis Antineoplastic Agents Catalysis Molecular Structure Stereoisomerism Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Catalysis |
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