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Molecules 2014, 19(2), 1544-1567; doi:10.3390/molecules19021544

Pharmacological Importance of Optically Active Tetrahydro-β-carbolines and Synthetic Approaches to Create the C1 Stereocenter

Laboratory of Organic Chemistry, Department of Chemistry, School of Chemical Tehcnology, Aalto University, PO Box 16100, Kemistintie 1, Aalto FI-00076, Finland
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Received: 19 December 2013 / Revised: 17 January 2014 / Accepted: 20 January 2014 / Published: 27 January 2014
(This article belongs to the Section Natural Products)

Abstract

1,2,3,4-Tetrahydro-β-carbolines (THβCs) are a pharmacologically important group of compounds belonging to the indole alkaloids. C1-Substituted optically active THβCs have been the target of extensive synthetic efforts due to the presence of the scaffold in numerous natural products and synthetic targets. This review briefly summarizes the methods to obtain the C1 stereocenter and concentrates on evaluating the pharmacological importance of optically active C1-substituted THβCs, including their PDE5-inhibitory, antimalarial, antiviral and antitumor activities.
Keywords: tetrahydro-β-carboline; THβC; pharmacological importance; biological activity; C1-substituted THβC tetrahydro-β-carboline; THβC; pharmacological importance; biological activity; C1-substituted THβC
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Laine, A.E.; Lood, C.; Koskinen, A.M.P. Pharmacological Importance of Optically Active Tetrahydro-β-carbolines and Synthetic Approaches to Create the C1 Stereocenter. Molecules 2014, 19, 1544-1567.

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