Design and synthesis of Tetrahydroindeno[4,5-c]chromen-4(3H)-one derivatives as antiproliferative agents for prostate Cancer cells

  • Bioorg Med Chem Lett. 2026 Apr:133:130515. doi: 10.1016/j.bmcl.2025.130515.
Hui-Yu Chan  1 ,  Pin-Shuo Huang  2 ,  Pei-Fang Chiu  2 ,  Tzung-Sheng Lin  2 ,  Li-Jou Huang  2 ,  Pi-Hui Liang  2 ,  Jih-Hwa Guh  2 ,  Mei-Hsiang Lin  3
Affiliations
  • 1. School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan; Department of Pharmacy, Changhua Christian Hospital, Changhua 500, Taiwan.
  • 2. School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
  • 3. School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan. Electronic address: [email protected].
PMID: 41453691 DOI: 10.1016/j.bmcl.2025.130515
Abstract

Abiraterone, a CYP17A1 Inhibitor, is approved by the FDA for castration-resistance prostate Cancer. To mimic the structure of abiraterone, we designed and synthesized nine tetrahydroindeno[4,5-c]chromen-4(3H)-one derivatives with pyridine congeners at C-1 position. Notably, 13c and 14c exhibited the GI50 of 10 nM against PC-3 cells compared to 21.4 μM for abiraterone. The docking studies further revealed that 14c shares a similar binding mode with abiraterone at the CYP17A1 active site.

Keywords
Abiraterone; Antiproliferation; Castration-resistance prostate cancer.
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