Privileged scaffolds for blocking protein–protein interactions: 1, 4-disubstituted naphthalene antagonists of transcription factor complex HOX–PBX/DNA

T Ji, M Lee, SC Pruitt, DG Hangauer

文献索引：Ji, Tao; Lee, Madison; Pruitt, Steven C.; Hangauer, David G. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 15 p. 3875 - 3879

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被引用次数: 9

摘要

Structure-based-design studies, with the crystal structure of the HOXB1–PBX1/DNA transcription factor complex, were used to identify 1, 4-disubstituted naphthalenes as potential antagonists. An initial library of 32 analogs was synthesized, two of which were found to be more potent than the reported activity for a 12 amino acid peptide antagonist. Antagonists were also identified of the related BRN1/DNA and BRN2/DNA transcription ...