Design, synthesis, in silico, and biological evaluation of novel pyrazolopyrimidinone-based estrogen receptor inhibitors

Key Points

• To design and evaluate new compounds that inhibit estrogen receptors and assess their potential against tumors with high estrogen levels.
• Synthesized novel pyrazolopyrimidinone compounds
• Conducted in silico evaluations for design and efficacy
• Performed biological evaluations in tumor models
• Compounds 5a and 5b exhibited significant inhibitory activity against high estrogen-expressing tumors