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W11, W12, and W23 are a series of functionalized lactams featuring four contiguous stereocenters, developed as potential small-molecule therapeutics for triple-negative breast cancer (TNBC). Identified through diversity-oriented synthesis, these compounds exhibit potent antiproliferative activity against aggressive TNBC cell lines such as MDA-MB-231, BT-549, and 4T1. Mechanistically, these lead candidates induce apoptosis and modulate reactive oxygen species (ROS) levels, leading to a significant reduction in cancer cell viability, clonogenicity, and motility. Preliminary pharmacokinetic profiling via SwissADME suggests favorable drug-like properties, including high gastrointestinal absorption, optimal lipophilicity, and Lipinski compliance, supporting their further development as targeted therapies for TNBC.
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