Discovery of Small-Molecule Inhibitors of the ATPase Activity of Human Papillomavirus E1 Helicase
Journal of Medicinal Chemistry2003Vol. 47(1), pp. 18–21
Citations Over TimeTop 10% of 2003 papers
Anne‐Marie Faucher, Peter W. White, Christian Brochu, Chantal Grand‐Maître, Jean Rancourt, Gulrez Fazal
Abstract
The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus E1 helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. This screen led to the discovery of (biphenyl-4-sulfonyl)acetic acid 1, which inhibits the ATPase activity of HPV type 6 E1 helicase with a low micromolar IC(50) value. A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series.
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