ArticleJournal of medicinal chemistry2015
Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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
10 citing papers in PubMed.
- Late-Stage Functionalization via Thianthrenation: A Reaction Enabling Rapid Preparation of Drug Beads for Chemical Pulldown.Journal of medicinal chemistry · 2026Article
- Optimization of Orally Bioavailable Antileishmanial 2,4,5-Trisubstituted Benzamides.Journal of medicinal chemistry · 2023Article
- Article
- Anti-Trypanosomal Proteasome Inhibitors Cure Hemolymphatic and Meningoencephalic Murine Infection Models of African Trypanosomiasis.Tropical medicine and infectious disease · 2020Article
- Screening of the Pathogen Box reveals new starting points for anti-trypanosomal drug discovery.MedChemComm · 2018Article
- Enantioselective radical process for synthesis of chiral indolines by metalloradical alkylation of diverse C(spChemical science · 2018Article
- Novel lead compounds in pre-clinical development against African sleeping sickness.MedChemComm · 2017Review
- Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery.Antimicrobial agents and chemotherapy · 2017Article
- Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.Bioorganic & medicinal chemistry · 2016Article
- Repurposing strategies for tropical disease drug discovery.Bioorganic & medicinal chemistry letters · 2016Review
Corrections and comments
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Authors and funding
14 authors.
Funding
Abstract
There is an urgent need for new, brain penetrant small molecules that target the central nervous system second stage of human African trypanosomiasis (HAT). We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypanosoma brucei from screening of a focused protease library against Trypanosoma brucei brucei in culture. We describe the optimization and characterization of this series. Potent antiproliferative activity was observed. The series demonstrated excellent pharmacokinetic properties, full cures in a stage 1 mouse model of HAT, and a partial cure in a stage 2 mouse model of HAT. Lack of tolerability prevented delivery of a fully curative regimen in the stage 2 mouse model and thus further progress of this series.
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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.