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Functionally Optimized Neuritogenic Farinosone C Analogs : SAR-Study and Investigations on Their Mode of Action

Burch, Patrick and Chicca, Andrea and Gertsch, Jürg and Gademann, Karl. (2014) Functionally Optimized Neuritogenic Farinosone C Analogs : SAR-Study and Investigations on Their Mode of Action. ACS medicinal chemistry letters, Vol. 5, H. 2. pp. 172-177.

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Official URL: http://edoc.unibas.ch/dok/A6337721

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Abstract

Several natural products derived from entomopathogenic fungi have been shown to initiate neuronal differentiation in the rat pheochromocytoma PC12 cell line. After the successful completion of the total synthesis program, the reduction of structural complexity while retaining biological activity was targeted. In this study, farinosone C served as a lead structure and inspired the preparation of small molecules with reduced complexity, of which several were able to induce neurite outgrowth. This allowed for the elaboration of a detailed structure-activity relationship. Investigations on the mode of action utilizing a computational similarity ensemble approach suggested the involvement of the endocannabinoid system as potential target for our analogs and also led to the discovery of four potent new endocannabinoid transport inhibitors.
Faculties and Departments:05 Faculty of Science > Departement Chemie > Former Organization Units Chemistry > Organische Chemie (Gademann)
UniBasel Contributors:Gademann, Karl
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:1948-5875
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:06 Mar 2015 07:44
Deposited On:06 Mar 2015 07:44

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