2026-10-14T13:55:58Z https://api.figshare.com/v2/oai

oai:figshare.com:article/34037136 2026-09-30T23:01:42Z category_4 category_7 category_19 category_21 category_272 category_873 category_734 category_61 category_64 portal_87 item_type_3 month_year_09_2026

Heterocyclic scaffolds targeting IDO1: progress in medicinal chemistry and clinical development Ankush Kumar (1458955) Vishakha Sharma (414810) Rajiv Patel (27201) Rajwinder Kaur (598597) Rohit Bhatia (767306) Biochemistry Medicine Pharmacology Biotechnology Environmental Sciences not elsewhere classified Chemical Sciences not elsewhere classified Biological Sciences not elsewhere classified Developmental Biology Cancer Biological activity cancer enzymatic assay IDO1 inhibitors SAR <p>This review mainly aims to systematically compile and analyze recently developed indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors reported over the past 5 years, with emphasis on heterocyclic scaffold-based classification, structure–activity relationships (SAR), and therapeutic relevance.</p> <p>A comprehensive literature survey was conducted to identify IDO1 inhibitors, which were categorized based on their core heterocyclic scaffolds. Studies involving biological evaluation, SAR analysis, and molecular docking were critically assessed.</p> <p>IDO1 inhibitors were classified into diverse scaffolds, including indoles, imidazoles, phenyl urea–benzimidazoles, azoles, imidazopyridines, benzofurans, quinolines, pyrimidines, erlotinib-based analogues, naphthoquinones, hydroxyamidine derivatives, quinazolines, and sulfonamide chromone-oxime analogues. Key SAR trends and biological activities were highlighted. Clinically investigated inhibitors such as indoximod, epacadostat, navoximod, LY3381916, linrodostat, and PF-06840003 were also evaluated for therapeutic outcomes.</p> <p>This review provides an updated overview of IDO1 inhibitor design and development, offering valuable insights into scaffold optimization and future directions for developing effective anticancer agents targeting tumor immunosuppression.</p> 2026-09-30T23:01:42Z Dataset Dataset 10.6084/m9.figshare.34037136.v1 https://figshare.com/articles/dataset/Heterocyclic_scaffolds_targeting_IDO1_progress_in_medicinal_chemistry_and_clinical_development/34037136 CC BY 4.0