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Russell F. Graceffa · SciRah

Researcher profile · Semantic Scholar

Russell F. Graceffa

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Russell F. Graceffa — researcher profile on SciRah

h-index: 16
Works: 22
Citations: 771

Most-cited papers

Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
J. Butera, Madelene M. Antane, Schuyler A. Antane, Thomas M. Argentieri +13 more
2000Journal of Medicinal Chemistry74 citations
Semantic Scholar
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
J. Harmange, M. Weiss, Julie Germain, A. Polverino +29 more
2008Journal of Medicinal Chemistry66 citations Open access
Semantic Scholar
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
Daniel S. La, J. Belzile, J. Bready, A. Coxon +20 more
2008Journal of Medicinal Chemistry65 citations Open access
Semantic Scholar
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
A. Gilbert, Madelene M. Antane, Thomas M. Argentieri, J. Butera +14 more
2000Journal of Medicinal Chemistry64 citations
Semantic Scholar
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Russell F. Graceffa, A. Boezio, J. Able, S. Altmann +40 more
2017Journal of Medicinal Chemistry62 citations Open access
Semantic Scholar
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.
Hong-Bing Huang, Daniel S. La, Alan C. Cheng, D. Whittington +13 more
2012Journal of Medicinal Chemistry57 citations Open access
Semantic Scholar
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
M. Weiss, Toni L. Williamson, S. Babu-Khan, M. Bartberger +34 more
2012Journal of Medicinal Chemistry56 citations Open access
Semantic Scholar
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
L. Schenkel, Philip R. Olivieri, A. Boezio, H. L. Deak +13 more
2016Journal of Medicinal Chemistry46 citations Open access
Semantic Scholar
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
M. Weiss, Thomas A. Dineen, Isaac E. Marx, S. Altmann +27 more
2017Journal of Medicinal Chemistry42 citations Open access
Semantic Scholar
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Thomas A. Dineen, M. Weiss, Toni L. Williamson, Paul D. Acton +37 more
2012Journal of Medicinal Chemistry40 citations Open access
Semantic Scholar
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
M. Weiss, J. Harmange, A. Polverino, D. Bauer +27 more
2008Journal of Medicinal Chemistry40 citations Open access
Semantic Scholar
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
E. A. Peterson, A. Boezio, P. Andrews, Christiane Boezio +22 more
2012Bioorganic & Medicinal Chemistry Letters35 citations Open access
Semantic Scholar
Direct, Regioselective N-Alkylation of 1,3-Azoles.
Shuai Chen, Russell F. Graceffa, A. Boezio
2016Organic Letters32 citations
Semantic Scholar
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
E. A. Peterson, P. Andrews, Xuhai Be, A. Boezio +18 more
2011Bioorganic & Medicinal Chemistry Letters28 citations Open access
Semantic Scholar
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.
Matthew R. Kaller, Scott S. Harried, B. Albrecht, P. Amarante +33 more
2012ACS Medicinal Chemistry Letters25 citations Open access
Semantic Scholar
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.
Daniel S. La, E. A. Peterson, C. Bode, A. Boezio +26 more
2017Bioorganic & Medicinal Chemistry Letters17 citations Open access
Semantic Scholar
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.
J. Allen, Matthew R. Lee, Chun-Ya E. Han, Jon Scherrer +9 more
2009Bioorganic & Medicinal Chemistry Letters11 citations Open access
Semantic Scholar
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.
A. Boezio, Kristin L. Andrews, Christiane Boezio, M. Chu-Moyer +15 more
2018Bioorganic & Medicinal Chemistry Letters9 citations Open access
Semantic Scholar
Synthesis and reactivity of cyclopentadienyltitanium complexes of the polydentate alkoxide ligand cis-1,3,5-cyclohexanetrialkoxide
D. Choquette, Wayne E. Buschmann, Russell F. Graceffa, R. Planalp
19952 citations
Semantic Scholar
P1-241 IN VIVO REDUCTION OF BETA-AMYLOID PEPTIDES IN THEBRAINOFTG2576MICEAFTER ORAL ADMINISTRATION OFA NOVEL BACE1 INHIBITOR
Juliette Jansson, Kristina Eliason, K. Kolmodin, Paul H. Wen +24 more
20190 citations
Semantic Scholar
Direct, Regioselective N‐Alkylation of 1,3‐Azoles.
Shuai Chen, Russell F. Graceffa, A. Boezio
20160 citations
Semantic Scholar
P1‐243: Pharmacokinetic and pharmacodynamic evaluation of orally available hydroxyethylamine‐derived beta‐secretase inhibitors in Sprague Dawley rats
Stephen Wood, Paul H. Wen, P. Amarante, Paul D. Acton +22 more
20120 citations Open access
Semantic Scholar

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