ArticleDrug development research2026
Antiplasmodial Activity and Pharmacokinetic Profiling of Cryptolepine and 2,7-Dibromocryptolepine With a View to Informing the Design of Novel Antimalarial Cryptolepine Analogues.
Article in Drug development research, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
1 citing paper in PubMed.
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Authors and funding
8 authors.
Funding
Abstract
The roots of the climbing shrub Cryptolepis sanguinolenta are traditionally used in West Africa for the treatment of malaria. The principal constituent, cryptolepine (1), has been shown to have antimalarial activity but there are concerns regarding its toxicity on account of its DNA-intercalating property. The synthetic analogue, 2,7-dibromocryptolepine, (2) does not intercalate into DNA and is markedly more active than the parent against Plasmodium sp. in vitro and in vivo. The aim of this study was to carry out a pre-clinical assessment of 1 and 2, and if appropriate, carry out in vivo pharmacokinetic studies. Cryptolepine (1) and 2,7-dibromocryptolepine (2), were evaluated in a range of in vitro assays in line with those recommended by Medicines for Malaria Venture (MMV) for the profiling of a Validated Hit Compound (https://www.mmv.org/frontrunner-templates). In vitro profiling of 1 and 2 showed that 2 is superior to 1 with respect to antiplasmodial activities, and the parasite rate of kill (fast for 2, in contrast with modest for 1); however 2 exhibited potent inhibition of the hERG potassium channel, (IC
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