ArticleACS medicinal chemistry letters2012
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The trial behind it
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Who cites it
22 citing papers in PubMed.
- Advances in high-throughput mass spectrometry in drug discovery.EMBO molecular medicine · 2023Review
- Ring Distortion of Vincamine Leads to the Identification of Re-Engineered Antiplasmodial Agents.ACS omega · 2021Article
- Synthesis of Polycyclic Ether-Benzopyrans and In Vitro Inhibitory Activity againstMolecules (Basel, Switzerland) · 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
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- The Importance of Collaboration between Industry, Academics, and Nonprofits in Tropical Disease Drug Discovery.ACS infectious diseases · 2018Article
- Discovery of Antimalarial Azetidine-2-carbonitriles That InhibitACS medicinal chemistry letters · 2017Article
- New developments in anti-malarial target candidate and product profiles.Malaria journal · 2017Review
- Article
- Novel diversity-oriented synthesis-derived respiratory syncytial virus inhibitors identified via a high throughput replicon-based screen.Antiviral research · 2016Article
- Diversity oriented synthesis for novel anti-malarials.Systems and synthetic biology · 2015Article
- Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.Cell · 2015Review
- Review
- Diversity-oriented synthesis probe targets Plasmodium falciparum cytochrome b ubiquinone reduction site and synergizes with oxidation site inhibitors.The Journal of infectious diseases · 2015Article
- Diversity-oriented synthesis and activity evaluation of substituted bicyclic lactams as anti-malarial against Plasmodium falciparum.Malaria journal · 2014Article
- Photoassisted diversity-oriented synthesis: accessing 2,6-epoxyazocane (oxamorphan) cores.The Journal of organic chemistry · 2014Article
- Diversity-oriented synthesis-facilitated medicinal chemistry: toward the development of novel antimalarial agents.Journal of medicinal chemistry · 2014Article
- Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification.Organic & biomolecular chemistry · 2014Review
- High content screening of diverse compound libraries identifies potent modulators of tubulin dynamics.ACS medicinal chemistry letters · 2014Article
- Rapid, scalable assembly of stereochemically rich, mono- and bicyclic acyl sultams.Organic letters · 2014Article
Corrections and comments
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Authors and funding
31 authors.
Funding
Abstract
Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synthesis (DOS) led to the initial hit. Structure-activity relationships guided the synthesis of compounds having improved potency and water solubility, yielding a subnanomolar inhibitor of parasite asexual blood-stage growth. Optimized compound 27 has an excellent off-target activity profile in erythrocyte lysis and HepG2 assays and is stable in human plasma. This compound is available via the molecular libraries probe production centers network (MLPCN) and is designated ML238.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.