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Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Eur J Med Chem. 2013 May; 63:299-312.EJ

Abstract

A series of 7,8-dehydrorutaecarpine derivatives were synthesized and characterized as potential multifunctional agents for treatment of Alzheimer's disease (AD). All of these synthetic compounds showed high acetylcholinesterase (AChE) inhibitory activity with IC50 values ranged from 0.60 to 196.7 nM, and good selectivity for AChE over butyrylcholinesterase (BuChE) (125- to 3225-fold). A Lineweaver-Burk plot and molecular modeling study indicated these compounds could bind to both catalytic active site and the peripheral anionic site of AChE. Besides, compounds showed higher activity of inhibiting AChE-induced amyloid-beta (Aβ) aggregation than curcumin, higher anti-oxidative activity than Trolox, and could also be good metal chelators. Considering their low cytotoxicity, our results indicated that these derivatives provide good templates for developing new multifunctional agents for AD treatment.

Authors+Show Affiliations

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23501115

Citation

He, Yan, et al. "Synthesis and Evaluation of 7,8-dehydrorutaecarpine Derivatives as Potential Multifunctional Agents for the Treatment of Alzheimer's Disease." European Journal of Medicinal Chemistry, vol. 63, 2013, pp. 299-312.
He Y, Yao PF, Chen SB, et al. Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. Eur J Med Chem. 2013;63:299-312.
He, Y., Yao, P. F., Chen, S. B., Huang, Z. H., Huang, S. L., Tan, J. H., Li, D., Gu, L. Q., & Huang, Z. S. (2013). Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. European Journal of Medicinal Chemistry, 63, 299-312. https://doi.org/10.1016/j.ejmech.2013.02.014
He Y, et al. Synthesis and Evaluation of 7,8-dehydrorutaecarpine Derivatives as Potential Multifunctional Agents for the Treatment of Alzheimer's Disease. Eur J Med Chem. 2013;63:299-312. PubMed PMID: 23501115.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. AU - He,Yan, AU - Yao,Pei-Fen, AU - Chen,Shuo-bin, AU - Huang,Zhi-hong, AU - Huang,Shi-Liang, AU - Tan,Jia-Heng, AU - Li,Ding, AU - Gu,Lian-Quan, AU - Huang,Zhi-Shu, Y1 - 2013/02/26/ PY - 2012/12/14/received PY - 2013/01/31/revised PY - 2013/02/13/accepted PY - 2013/3/19/entrez PY - 2013/3/19/pubmed PY - 2013/12/16/medline SP - 299 EP - 312 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 63 N2 - A series of 7,8-dehydrorutaecarpine derivatives were synthesized and characterized as potential multifunctional agents for treatment of Alzheimer's disease (AD). All of these synthetic compounds showed high acetylcholinesterase (AChE) inhibitory activity with IC50 values ranged from 0.60 to 196.7 nM, and good selectivity for AChE over butyrylcholinesterase (BuChE) (125- to 3225-fold). A Lineweaver-Burk plot and molecular modeling study indicated these compounds could bind to both catalytic active site and the peripheral anionic site of AChE. Besides, compounds showed higher activity of inhibiting AChE-induced amyloid-beta (Aβ) aggregation than curcumin, higher anti-oxidative activity than Trolox, and could also be good metal chelators. Considering their low cytotoxicity, our results indicated that these derivatives provide good templates for developing new multifunctional agents for AD treatment. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/23501115/Synthesis_and_evaluation_of_78_dehydrorutaecarpine_derivatives_as_potential_multifunctional_agents_for_the_treatment_of_Alzheimer's_disease_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(13)00108-6 DB - PRIME DP - Unbound Medicine ER -