ArticleEuropean journal of medicinal chemistry2021
Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
Article in European journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 34 citations in OpenAlex.
- Large-Scale Chemical-Genetic Interaction Profiling Identifies a Small-Molecule Inhibitor ofACS infectious diseases · 2026Article
- The Biosynthetic Pathway of Mycolic Acids: Dual-Function Targets for Tuberculosis Therapeutics and Green Steroid Drugs Biomanufacturing.Pharmaceutics · 2025Review
- Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies.Journal of medicinal chemistry · 2025Review
- Synthesis and evaluation of Trehalose-Pks13 inhibitor conjugates targeting mycobacteria.Carbohydrate research · 2025Article
- Discovery of 2,4,5-Substituted Benzoxazole Derivatives as Pks13 Inhibitors via the Scaffold Hopping Strategy.ACS infectious diseases · 2025Article
- Copper(I)-Catalyzed Intramolecular Tandem Acylation/The Journal of organic chemistry · 2025Article
- Inhibitors of the Thioesterase Activity ofACS infectious diseases · 2024Article
- Unlocking Opportunities forACS infectious diseases · 2024Review
- Polyketide Synthase 13 (Pks13) Inhibition: A Potential Target for New Class of Anti-tubercular Agents.Current topics in medicinal chemistry · 2024Review
- Synthesis of Benzothiophene-3-carboxylic Esters by Palladium Iodide-Catalyzed Oxidative Cyclization-Deprotection-Alkoxycarbonylation Sequence under Aerobic Conditions.The Journal of organic chemistry · 2023Article
- Synthesis of tetrahydrofuro[3,2-Beilstein journal of organic chemistry · 2023Article
- OvercomingActa pharmaceutica Sinica. B · 2022Review
- Design, Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2022Article
- Anti-tuberculosis drug developmentFrontiers in microbiology · 2022Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
Abstract
We previously reported a series of coumestans-a naturally occurring tetracyclic scaffold containing a δ-lactone-that effectively target the thioesterase domain of polyketide synthase 13 (Pks13) in Mycobacterium tuberculosis (Mtb), resulting in superior anti-tuberculosis (TB) activity. Compared to the corresponding 'open-form' ethyl benzofuran-3-carboxylates, the enhanced anti-TB effects seen with the conformationally restricted coumestan series could be attributed to the extra π-π stacking interactions between the benzene ring of coumestans and the phenyl ring of F1670 residue located in the Pks13-TE binding domain. To further probe this binding feature, novel tetracyclic analogues were synthesized and evaluated for their anti-TB activity against the Mtb strain H
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Registered trials
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