ArticleInternational journal for parasitology. Drugs and drug resistance2016
Spirocyclic chromanes exhibit antiplasmodial activities and inhibit all intraerythrocytic life cycle stages.
Article in International journal for parasitology. Drugs and drug resistance, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Eschweilenol C and subfractions from Terminalia plants disrupt haemoglobin metabolism, inhibiting Plasmodium falciparum growth at rings and trophozoite stages.Malaria journal · 2025Article
- Sulfonamide based pyrimidine derivatives combatingRSC advances · 2024Article
- Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity.Bioorganic & medicinal chemistry · 2022Article
- Ring Distortion of Vincamine Leads to the Identification of Re-Engineered Antiplasmodial Agents.ACS omega · 2021Article
- Synthesis and Structural Characterization of 1-(ACS omega · 2021Article
- Antiplasmodial Compounds from Deep-Water Marine Invertebrates.Marine drugs · 2021Article
- Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.Journal of medicinal chemistry · 2020Article
- Re-Engineering of Yohimbine's Biological Activity through Ring Distortion: Identification and Structure-Activity Relationships of a New Class of Antiplasmodial Agents.ACS infectious diseases · 2020Article
- DeepMalaria: Artificial Intelligence Driven Discovery of Potent Antiplasmodials.Frontiers in pharmacology · 2019Article
- 4-Nitro styrylquinoline is an antimalarial inhibiting multiple stages of Plasmodium falciparum asexual life cycle.International journal for parasitology. Drugs and drug resistance · 2017Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
We screened a collection of synthetic compounds consisting of natural-product-like substructural motifs to identify a spirocyclic chromane as a novel antiplasmodial pharmacophore using an unbiased cell-based assay. The most active spirocyclic compound UCF 201 exhibits a 50% effective concentration (EC50) of 350 nM against the chloroquine-resistant Dd2 strain and a selectivity over 50 using human liver HepG2 cells. Our analyses of physicochemical properties of UCF 201 showed that it is in compliance with Lipinski's parameters and has an acceptable physicochemical profile. We have performed a limited structure-activity-relationship study with commercially available chromanes preserving the spirocyclic motif. Our evaluation of stage specificities of UCF 201 indicated that the compound is early-acting in blocking parasite development at ring, trophozoite and schizont stages of development as well as merozoite invasion. SPC is an attractive lead candidate scaffold because of its ability to act on all stages of parasite's aexual life cycle unlike current antimalarials.
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