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Synthesis of Diverse Lactam Carboxamides Leading to the Discovery of a New Transcription‐Factor Inhibitor
Author(s) -
Ng Pui Yee,
Tang Yuchen,
Knosp Wendy M.,
Stadler H. Scott,
Shaw Jared T.
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200700762
Subject(s) - transcription factor , transcription (linguistics) , lactam , computational biology , diversity (politics) , common core , chemistry , dna , biology , bioinformatics , combinatorial chemistry , stereochemistry , biochemistry , computer science , gene , core (optical fiber) , philosophy , linguistics , sociology , anthropology , telecommunications
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.