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March 31, 2026Anti-Cancer Agents in Medicinal Chemistry

Sulfonamides as Aromatase Inhibitors: Nimesulide Analogues, N-cyclic- and Aryl-Sulfonamides

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Authors

CMCristina MaccalliniAAAlessandra AmmazzalorsoBFBarbara De Filippis

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Overview

This review discusses sulfonamide-based aromatase inhibitors and their enzyme interactions, emphasizing structural relationships.

Key Points

  • The review aims to analyze structure–activity relationships of nonsteroidal aromatase inhibitors with sulfonamide groups.
  • Literature review of existing sulfonamide-based aromatase inhibitors
  • Classification based on core scaffold: nimesulide analogues, N-cyclic sulfonamides, aryl-sulfonamides
  • Evaluation of biological results related to enzyme inhibition
  • Molecular modeling to assess interactions with active-site residues of aromatase.
  • Identified significant structure–activity relationships for sulfonamide-containing aromatase inhibitors.
  • Demonstrated effective enzyme inhibition through hydrogen bonding interactions.
  • Highlighted the importance of hydrophobic groups and aromatic rings in binding affinity.

Cite This Study

Maccallini et al. (2026) studied this question.

synapsesocial.com/papers/69cb6541e6a8c024954b9506https://doi.org/10.2174/0118715206416396251122063142
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Also Consider

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  1. 1Discovery and Evaluation of Novel Sulfonamide Derivatives Targeting Aromatase in ER+ Breast Cancer2025 · 3 citations
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  3. 3Ligand and Structure-Based Drug Design of Biphenyl 1,2,4-Triazole Derivatives as Dual Target Inhibitors of Aromatase and Steroidal Sulfatase as Anti-Breast Cancer Agents2026
  4. 4Structure‐Guided Identification of Novel Aromatase Inhibitors Targeting Breast Carcinoma2024
  5. 5Design, Synthesis and Molecular Modeling Studies of Triazole Derivatives as Aromatase İnhibitors2026