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.
Highlights
Laboratory of Organic Chemistry, Department of Chemistry, School of Chemical Tehcnology, Aalto University, PO Box 16100, Kemistintie 1, Aalto FI-00076, Finland; Tel.: +358-50-555-3310
1,2,3,4-Tetrahydro-β-carbolines (THβCs), a compound class within the indole alkaloids, consist of a variety of both simple and complex natural and synthetic compounds [1]. These compounds possess a vast spectrum of biological activities and their use in novel pharmacological applications is under constant study, as the THβC structure is present in drugs currently available on the market, drug candidates under development and many other pharmacologically interesting compounds [2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17]
C1-Substituted THβCs have a wide variety of pharmacological properties, including phosphodiesterase 5 (PDE5)-inhibitory [2], antimalarial [3,4,5,6,7,8,9], antiviral [10,11,12,13] and antitumor [14,15,16,17] activities
Summary
1,2,3,4-Tetrahydro-β-carbolines (THβCs), a compound class within the indole alkaloids, consist of a variety of both simple and complex natural and synthetic compounds [1]. These compounds possess a vast spectrum of biological activities and their use in novel pharmacological applications is under constant study, as the THβC structure is present in drugs currently available on the market, drug candidates under development and many other pharmacologically interesting compounds [2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17]. The best known natural THβCs have been isolated from Peganum harmala and Pausinystalia yohimbe (formerly Corynathe yohimbe) Yohimbe alkaloids encompass such pharmacologically interesting natural products as yohimbine and its isomers, reserpine and ajmalicine (Figure 2) the latter two being currently used as antihypertensive drugs. Tadalafil is used for pulmonary arterial hypertension treatment under the brand name Adcirca
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