ArticleJournal of medicinal chemistry2020
Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors.
Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 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
32 citing papers in PubMed, 62 citations in OpenAlex.
- Ligand-mediated conformation diversity of Hsp90 revealed by GaMD simulations and Markov model.Molecular diversity · 2026Article
- Structural Insights into Selectively TargetingBiochemistry · 2025Article
- Is a Fungal Apocalypse Inevitable or Just a Hallucination? An Overview of the Antifungal Armamentarium Used in the Fight against Pathogenic Fungi.ACS medicinal chemistry letters · 2025Review
- The Significance of Mono- and Dual-Effective Agents in the Development of New Antifungal Strategies.Chemical biology & drug design · 2025Review
- The progress and future of the treatment of Candida albicans infections based on nanotechnology.Journal of nanobiotechnology · 2024Review
- Interdisciplinary approaches for the discovery of novel antifungals.Trends in molecular medicine · 2024Review
- FRET Assays for the Identification ofPharmaceuticals (Basel, Switzerland) · 2024Article
- Advancements and challenges in antifungal therapeutic development.Clinical microbiology reviews · 2024Review
- SynergisticFrontiers in cellular and infection microbiology · 2024Article
- Various Biomimetics, Including Peptides as Antifungals.Biomimetics (Basel, Switzerland) · 2023Review
- Roles of Hsp90 in Candida albicans morphogenesis and virulence.Current opinion in microbiology · 2023Review
- Functional genomic analysis ofiScience · 2023Article
- Article
- Combating increased antifungal drug resistance inActa biochimica et biophysica Sinica · 2023Review
- Drug Target Elucidation Through Isolation and Analysis of Drug-Resistant Mutants in Cryptococcus neoformans.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Antifungal discovery.Current opinion in microbiology · 2022Review
- Genomic Approaches to Antifungal Drug Target Identification and Validation.Annual review of microbiology · 2022Review
- The role ofiScience · 2022Review
- Chemical Chaperones to Inhibit Endoplasmic Reticulum Stress: Implications in Diseases.Drug design, development and therapy · 2022Review
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
Abstract
The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence, and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen's human host, preventing the use of known clinical Hsp90 inhibitors in antifungal applications due to concomitant host toxicity issues. With the goal of developing Hsp90 inhibitors with acceptable therapeutic indices for the treatment of invasive fungal infections, we initiated a program to design and synthesize potent inhibitors with selective activity against fungal Hsp90 isoforms over their human counterparts. Building on our previously reported derivatization of resorcylate natural products to produce fungal-selective compounds, we have developed a series of synthetic aminopyrazole-substituted resorcylate amides with broad, potent, and fungal-selective Hsp90 inhibitory activity. Herein we describe the synthesis of this series, as well as biochemical structure-activity relationships driving selectivity for the Hsp90 isoforms expressed by
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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.