Lead optimization of 5jc21 (CG13250), a quinolin-2(1 H )-one-based inhibitor of the BRD4 member of the bromodomain and extraterminal (BET) family of proteins

Key Points

• The research aims to optimize the lead compound 5jc21 for enhanced inhibition of BRD4, a key target in cancer therapy.
• Conducted lead optimization for 5jc21, a quinolin-2(1H)-one derivative.
• Evaluated BRD4 inhibition potency of synthesized compounds in vitro.
• Assessed structure-activity relationships to enhance efficacy.
• 5jc21 demonstrated significant BRD4 inhibitory activity in preliminary assessments.
• Enhanced potency observed with 4,6-disubstituted quinolinones compared to previous iterations.