Journal of Medicinal Chemistry · 2003 · 114 citations · 2 references
PharmacyBiochemistryMedicinal ChemistryDrug DiscoveryMolecular VirologyVirologyAntiviral TherapyEnzyme InhibitionHit-to-lead OptimizationHuman Papillomavirus InfectionLead Compound DesignLead DiscoveryAntiviral TherapeuticsHpv PathogenesisHuman Papillomavirus ScreeningLead Enzyme DiscoveryPapillomavirus BiologyViral Helicase Inhibitors
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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The Design of Leadlike Combinatorial Libraries
Simon J. Teague, A. M. Davis, Paul D. Leeson et al. · Angewandte Chemie International Edition · 1999 · 810 citations