Synthesis of Diverse Lactam Carboxamides Leading to the Discovery of a New Transcription‐Factor Inhibitor

Diversity is the key: Skeletal diversity is a useful starting point in the search for compounds that modulate protein–biopolymer interactions. A library of 400 lactam carboxamides has been synthesized in a short synthetic sequence and a new compound that inhibits the interaction of a transcription factor (HOXA13) with its DNA target has been discovered, and inhibition of transcription is demonstrated in cells.