Publications by authors named "David Frennesson"

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Potent Long-Acting Inhibitors Targeting the HIV-1 Capsid Based on a Versatile Quinazolin-4-one Scaffold.
Eric P Gillis, Kyle Parcella, Michael Bowsher, James H Cook, Christiana Iwuagwu, David B Frennesson

J Med Chem· February 2023

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The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Chetan Padmakar Darne, Upender Velaparthi, Mark Saulnier, David Frennesson, Peiying Liu

Bioorg Med Chem Lett· November 2022

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Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.
Kyle Parcella, Tao Wang, Kyle Eastman, Zhongxing Zhang, Zhiwei Yin, David Frennesson

ACS Med Chem Lett· June 2022

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5-Bromo-2-chloro-4-fluoro-3-iodopyridine as a Halogen-rich Intermediate for the Synthesis of Pentasubstituted Pyridines.
Yong-Jin Wu, Gerard J Porter, David B Frennesson, Mark G Saulnier

J Org Chem· March 2022

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Biochemical and transcriptional profiling to triage additional activities in a series of IGF-1R/IR inhibitors.
Petra Ross-Macdonald, Heshani de Silva, Vishal Patel, Amy Truong, Aiqing He, David Frennesson

Bioorg Med Chem· March 2012

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Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Upender Velaparthi, Mark G Saulnier, Mark D Wittman, Peiying Liu, David B Frennesson

Bioorg Med Chem Lett· May 2010

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SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Kurt Zimmermann, Mark D Wittman, Mark G Saulnier, Upender Velaparthi, Xiaopeng Sang, David B Frennesson

Bioorg Med Chem Lett· March 2010

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Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Mark D Wittman, Joan M Carboni, Zheng Yang, Francis Y Lee, Melissa Antman, David Frennesson

J Med Chem· December 2009

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Nucleophilic capture of the imino-quinone methide type intermediates generated from 2-aminothiazol-5-yl carbinols.
Mark G Saulnier, Marco Dodier, David B Frennesson, David R Langley, Dolatrai M Vyas

Org Lett· November 2009

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Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Kurt Zimmermann, Mark D Wittman, Mark G Saulnier, Upender Velaparthi, David R Langley, David Frennesson

Bioorg Med Chem Lett· July 2008

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2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Mark G Saulnier, David B Frennesson, Mark D Wittman, Kurt Zimmermann, Upender Velaparthi

Bioorg Med Chem Lett· March 2008

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In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417.
Paul Haluska, Joan M Carboni, David A Loegering, Francis Y Lee, Mark Wittman, David B Frennesson

Cancer Res· January 2006

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Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Mark Wittman, Joan Carboni, Ricardo Attar, Balu Balasubramanian, Praveen Balimane, David Frennesson

J Med Chem· September 2005

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Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
Mark G Saulnier, Balu N Balasubramanian, Byron H Long, David B Frennesson, Edward Ruediger

J Med Chem· April 2005

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Novel 3',6'-anhydro and N12,N13-bridged glycosylated fluoroindolo[2,3-a]carbazoles as topoisomerase I inhibitors. Fluorine as a leaving group from sp3 carbon.
Mark G Saulnier, David R Langley, David B Frennesson, Byron H Long, Stella Huang

Org Lett· March 2005

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Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-beta-D-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model.
Balu N Balasubramanian, Denis R St Laurent, Mark G Saulnier, Byron H Long, Carol Bachand, David B Frennesson

J Med Chem· March 2004

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