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

Abstract

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. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2007/z700762_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.