ArticleJournal of medicinal chemistry2019
Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Challenges of Aufheben to Promote Druglikeness: Chemical Modification Strategies to Improve Aqueous Solubility and Permeability.Journal of medicinal chemistry · 2025Review
- Identification of Substituted 4-Aminocinnolines as Broad-Spectrum Antiparasitic Agents.ACS infectious diseases · 2025Article
- Exploration of innovative drug repurposing strategies for combating human protozoan diseases: Advances, challenges, and opportunities.Journal of pharmaceutical analysis · 2025Review
- Evolution of the Quinoline Scaffold for the Treatment of Leishmaniasis: A Structural Perspective.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Multiparameter ranking of carbazoles for anti-trypanosome lead discovery.Frontiers in drug discovery · 2024Article
- 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure-property relationships and key biological targets.Frontiers in chemistry · 2024Review
- Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy.Journal of medicinal chemistry · 2023Article
- Development of Combretastatin A-4 Analogues as Potential Anticancer Agents with Improved Aqueous Solubility.Molecules (Basel, Switzerland) · 2023Article
- Chemical Optimization of CBL0137 for Human African Trypanosomiasis Lead Drug Discovery.Journal of medicinal chemistry · 2023Article
- Identification of novel anti-amoebic pharmacophores from kinase inhibitor chemotypes.Frontiers in microbiology · 2023Article
- Hypothesis-generating proteome perturbation to identify NEU-4438 and acoziborole modes of action in the African Trypanosome.iScience · 2022Article
- How Physiologic Targets Can Be Distinguished from Drug-Binding Proteins.Molecular pharmacology · 2021Article
- Biological Evaluation and Mechanistic Studies of Quinolin-(1Antimicrobial agents and chemotherapy · 2021Article
- Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead forJournal of medicinal chemistry · 2020Article
- Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.ACS medicinal chemistry letters · 2020Article
- Structure-Bioactivity Relationships of Lapatinib Derived Analogs againstACS medicinal chemistry letters · 2020Article
- Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-Journal of medicinal chemistry · 2020Article
Corrections and comments
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Authors and funding
16 authors.
Funding
Abstract
Lapatinib, an approved epidermal growth factor receptor inhibitor, was explored as a starting point for the synthesis of new hits against Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). Previous work culminated in 1 (NEU-1953), which was part of a series typically associated with poor aqueous solubility. In this report, we present various medicinal chemistry strategies that were used to increase the aqueous solubility and improve the physicochemical profile without sacrificing antitrypanosomal potency. To rank trypanocidal hits, a new assay (summarized in a cytocidal effective concentration (CEC
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