Design and synthesis of Tetrahydroindeno[4,5-c]chromen-4(3H)-one derivatives as antiproliferative agents for prostate Cancer cells.
Journal
Bioorganic and Medicinal Chemistry Letters
Journal Volume
133
Start Page
130515
ISSN
1464-3405
Date Issued
2026-04
Author(s)
Chan, Hui-Yu
Huang, Pin-Shuo
Chiu, Pei-Fang
Lin, Tzung-Sheng
Huang, Li-Jou
Lin, Mei-Hsiang
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 GI 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.
Subjects
Abiraterone
Antiproliferation
Castration-resistance prostate cancer
Type
journal article