Francis Beaulieu | Researchain

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Featured researches published by Francis Beaulieu.

Bioorganic & Medicinal Chemistry Letters | 2015

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

B. Narasimhulu Naidu; Margaret E. Sorenson; Manoj Patel; Yasutsugu Ueda; Jacques Banville; Francis Beaulieu; Sagarika Bollini; Ira B. Dicker; Helen Higley; Zeyu Lin; Lori Pajor; Dawn D. Parker; Brian Terry; Ming Zheng; Alain Martel; Nicholas A. Meanwell; Mark Krystal; Michael A. Walker

Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and pharmacokinetic profiles of several C2-carbon-linked heterocyclic pyrimidinone-4-carboxamides that inhibit the strand transfer step of the integration process.

Bioorganic & Medicinal Chemistry Letters | 2016

Pyridoxine hydroxamic acids as novel HIV-integrase inhibitors.

Brent Richard Stranix; Jinzi J. Wu; Guy Milot; Francis Beaulieu; Jean-Emanuel Bouchard; Kristine Gouveia; André J. Forté; Seema Garde; Zhigang Wang; Jean-François Mouscadet; Olivier Delelis; Yong Xiao

A series of pyridoxine hydroxamic acid analog bearing a 5-aryl-spacers were synthesized. Evaluation of these novel HIV integrase complex inhibitors revealed compounds with high potency against wild-type HIV virus.

Journal of Medicinal Chemistry | 2005

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 D. Wittman; Joan M. Carboni; Ricardo M. Attar; Balu Balasubramanian; Praveen Balimane; Patrick Brassil; Francis Beaulieu; Chiehying Chang; Wendy Clarke; Janet Dell; Jeffrey Eummer; David B. Frennesson; Marco M. Gottardis; Ann Greer; Steven Hansel; Warren Hurlburt; Bruce L. Jacobson; Subramaniam Krishnananthan; Francis Y. Lee; Aixin Li; Tai-An Lin; Peiying Liu; Carl Ouellet; Xiaopeng Sang; Mark G. Saulnier; Karen Stoffan; Yax Sun; Upender Velaparthi; Henry Wong; Zheng Yang

Bioorganic & Medicinal Chemistry Letters | 2007

Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors

Francis Beaulieu; Carl Ouellet; Edward H. Ruediger; Makonen Belema; Yuping Qiu; Xuejie Yang; Jacques Banville; James R. Burke; Kurt R. Gregor; John F. MacMaster; Alain Martel; Kim W. McIntyre; Mark A. Pattoli; F. Christopher Zusi; Dolatrai M. Vyas

Bioorganic & Medicinal Chemistry Letters | 2007

Synthesis and structure-activity relationship of imidazo (1,2 -a )thieno (3,2 -e )pyrazines as IKK-β inhibitors

Makonen Belema; Amy Bunker; Van N. Nguyen; Francis Beaulieu; Carl Ouellet; Yuping Qiu; Yunhui Zhang; Alain Martel; James R. Burke; Kim W. McIntyre; Mark A. Pattoli; Connie Daloisio; Kathleen M. Gillooly; Wendy Clarke; Patrick J. Brassil; F. Chris Zusi; Dolatrai M. Vyas

Journal of Medicinal Chemistry | 2005

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 Balasubramanian; Byron H. Long; David B. Frennesson; Edward H. Ruediger; Kurt Zimmermann; Jeffrey Eummer; Denis R. St. Laurent; Karen Stoffan; B. Narasimhulu Naidu; Mikael Mahler; Francis Beaulieu; Carol Bachand; Frank Y. Lee; Craig R. Fairchild; Linda K. Stadnick; William C. Rose; Carola Solomon; Henry Wong; Alain Martel; John J. Wright; Robert Kramer; David R. Langley; Dolatrai M. Vyas

Archive | 2005

Bicyclic heterocycles as hiv integrase inhibitors

B. Narasimhulu Naidu; Jacques Banville; Francis Beaulieu; Timothy P. Connolly; Mark Krystal; John D. Matiskella; Carl Ouellet; Serge Plamondon; Roger Remillard; Margaret E. Sorenson; Yasutsugu Ueda; Michael A. Walker

Journal of Medicinal Chemistry | 2004

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-β- 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 Balasubramanian; Denis R. St. Laurent; Mark G. Saulnier; Byron H. Long; Carol Bachand; Francis Beaulieu; Wendy Clarke; Milind Deshpande; Jeffrey Eummer; Craig R. Fairchild; David B. Frennesson; Robert Kramer; Frank Y. Lee; Mikael Mahler; Alain Martel; B. Narasimhulu Naidu; William C. Rose; John W. Russell; Edward H. Ruediger; Carola Solomon; Karen Stoffan; Henry Wong; Kurt Zimmermann; Dolatrai M. Vyas

Archive | 2003

Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same

Makonen Belema; Amy Bunker; Van N. Nguyen; Francis Beaulieu; Carl Ouellet; Anne Marinier; Stephan Roy; Xuejie Yang; Yuping Qiu; Yunhui Zhang; Alain Martel; Christopher Zusi

Archive | 2001