ArticleACS medicinal chemistry letters2024
New Structural Features of Isatin Dihydrothiazole Hybrids for Selective Carbonic Anhydrase Inhibitors.
Article in ACS medicinal chemistry letters, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- One-Pot Synthesis of Dihydrothiazole-Hydrazone Hybrids and Evaluation of Their Absorption and Emission Properties.Journal of fluorescence · 2026Article
- Dynamic Evolution of the Tumor Immune Microenvironment in Malignant Tumors and Emerging Therapeutic Paradigms.MedComm · 2025Review
- Unraveling the Potential of Amino‑, Acylamino‑, and Ureido-Substituted 3ACS medicinal chemistry letters · 2025Article
- Synthesis and Evaluation of Thiazolidinone-Isatin Hybrids for Selective Inhibition of Cancer-Related Carbonic Anhydrases.ACS medicinal chemistry letters · 2025Article
- Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors.Molecules (Basel, Switzerland) · 2024Article
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chemotherapeutic agents have remained the first-line treatment option for advanced-stage cancers when surgery or radiation therapy is not viable. Human carbonic anhydrase (hCA) isoforms IX and XII have been validated as anticancer targets. In particular, hCA IX is overexpressed in several solid tumor cells. As a result, selective isoform inhibitors with high potency and low toxicity are sought after. Pursuing our investigation on new scaffolds as hCA-selective inhibitors, a new series of isatin thiazolidinone hybrids has been designed and synthesized. Their biological activity and selectivity toward hCA I, hCA II, hCA IX, and hCA XII were investigated. The results revealed an inhibitory activity in the nanomolar range on carbonic anhydrases IX and XII, and the nature of substitution in positions 3 and 5 of thiazolidinone appears to be crucial for the compounds' selectivity. Docking experiments have been applied to predict the binding mode of these new, promising derivatives.
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Registered trials
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