Med. Chem. Res. 2023, Vol 32, Iss 7

Med. Chem. Res. 2023, Vol 32, Iss 7

Medicinal Chemistry Research | 2023 | ?Volume 32, Issue 7, ?is now available online.

Special Issue in Honor of Dr. Nicholas A. Meanwell on the Occasion of His Retirement from Bristol Myers Squibb

In this issue

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Editorial

Special issue of Medicinal Chemistry Research in honor of Dr. Nicholas A. Meanwell

John F. Kadow, Kap-Sun Yeung, T. G. Murali Dhar

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Featured Biography

Reflections on a 40-year career in drug design and discovery

Nicholas A. Meanwell

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Comment

Future challenges and opportunities with fluorine in drugs?

David O’Hagan, Robert J. Young

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Comment

Toxicology Modernization: Misnomer or Momentum

Lois Lehman-McKeeman, Myrtle Davis

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Review Article

Successes in antiviral drug discovery: a tribute to Nick Meanwell

David P. Rotella

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Review Article

Acyl glucuronides–mediators of drug-induced toxicities?

Thomas A. Baillie

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Review Article

C-C bond cleavage reactions catalyzed by cytochrome P450 enzymes

F. Peter Guengerich, Yasuhiro Tateishi, Kevin D. McCarty

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Review Article

Harnessing the necessary nitrogen atom in chemical biology and drug discovery

Lewis D. Pennington, Philip N. Collier, Eamon Comer

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Review Article

The rise of targeting chimeras (TACs): next-generation medicines that preempt cellular events

Scott Hollingsworth, Scott Johnson, Pouyan Khakbaz, Yilin Meng, Varnavas Mouchlis, Olivia Pierce, Vera Prytkova, Erik Vik, Dahlia Weiss, Veerabahu Shanmugasundaram

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Review Article

A guide for the synthesis of key nucleoside scaffolds in drug discovery

Dinithi G. Rajapaksha, Subhojit Mondal, Jason W. Wang, Michael W. Meanwell

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Review Article

Targeting MDM2 for the development of a new cancer therapy: progress and challenges

Angelo Aguilar, Junius E. Thomas, Shaomeng Wang

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Review Article

The HBV capsid modulators derived from sulfamoylbenzamides and benzamides: an overview of the progress of patents

Nicky Hwang, Jason A. Clement, Ju-Tao Guo, Yanming Du

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Brief Report

Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain

Carolyn D. Dzierba, Bireshwar Dasgupta, George Karageorge, Walter Kostich, Brian Hamman, Jason Allen, Kim M. Esposito, Ramesh Padmanabha, James Grace, Kimberley Lentz, John Morrison, Daniel Morgan, Amy Easton, Clotilde Bourin, Marc R. Browning, Ramkumar Rajamani, Andrew Good, Dawn D. Parker, Jodi K. Muckelbauer, Javed Khan, Daniel Camac, Kaushik Ghosh, Vivek Halan, Jonathan S. Lippy, Kenneth S. Santone, R. Rex Denton, Ryan Westphal, Linda J. Bristow, Charles M. Conway, Joanne J. Bronson, John E. Macor

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Brief Report

Synthetic studies toward a simplified eleuthoside core

Paul M. Scola, John F. Kadow, David Langley, Dolatrai Vyas

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Brief Report

SARS-CoV-2 3CL-protease inhibitors derived from ML300: investigation of P1 and replacements of the 1,2,3-benzotriazole

Alice Hooper, Jonathan D. Macdonald, Brenna Reilly, Joshua Maw, Aidan P. Wirrick, Sang Hoon Han, A. Abigail Lindsey, Emma G. Rico, Todd Romigh, Christopher M. Goins, Nancy S. Wang, Shaun R. Stauffer

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Brief Report

Development of convenient crystallization inhibition assays for structure-activity relationship studies in the discovery of crystallization inhibitors

Jeffrey Yang, Haifa Albanyan, Yiling Wang, Yanhui Yang, Amrik Sahota, Longqin Hu

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Original Research

Novel potent and highly selective DDR1 inhibitors from integrated lead finding

Bernd Kuhn, Martin Ritter, J?rg Benz, Buelent Kocer, Jér?me C. Sarie, Remo Hochstrasser, Markus G. Rudolph, Shojiro Kadono, Tetsu Matsuura, Takeshi Murata, Hans Richter, Marco Prunotto

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Original Article

Structure-based optimization of aminothiadiazole inhibitors of AKT

Deborah S. Mortensen, Sayee G. Hegde, Sophie M. Perrin-Ninkovic, Sogole Bahmanyar, Meg McCarrick, Roy Harris, Robert Hilgraf, Branden G. S. Lee, Jeff McKie, Lisa Nadolny, John Sapienza, Alice Collette, Sarah Cox, James C. Gamez, Jennifer L. Hensel, Xuequn Helen Hua, Jim Leisten, Heather K. Raymon, Tam Tran, Rama Krishna Narla

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Original Article

Amide- and bis-amide-linked highly potent and broadly active antifungal agents for the treatment of invasive fungal infections- towards the discovery of pre-clinical development candidate FC12406

Simon D. P. Baugh, Anna Chaly, Damian G. Weaver, David B. Whitman, Jeffrey C. Pelletier, Haiyan Bian, Katie B. Freeman, Allen B. Reitz, Richard W. Scott

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Original Article

Discovery and exploration of monosaccharide linked dimers of galectin-3 inhibitors to target fibrosis

Jacob J. Swidorski, Brett R. Beno, Chunjian Liu, David S. Yoon, Kaushik Ghosh, Harinath Sale, Devang Shah, Kriti Acharya, Joseph Yanchunas, Priyanka Haldar, Narasimharaju Kalidindi, Jinal K. Shukla, Matthew Argentieri, Bruce A. Ellsworth, Dong Cheng, Alicia Regueiro-Ren

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Original Article

A versatile strategy for the synthesis of various lumazine peptides

Wanli Zhang, Andrew R. Mahoney, Michelle Garrison, William M. Wuest

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Original Article

Pharmacophore variants of the macrocyclic peptide triazole inactivator of HIV-1 Env

Monisha Gupta, Gabriela Canziani, Charles Ang, Mohammadjavad Mohammadi, Cameron F. Abrams, Derek Yang, Amos B. Smith, Irwin Chaiken

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Original Research Article

Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→π*Ar interaction

Paul M. Wehn, Song Yang, Jonas A. Grina, James P. Rizzi, Stephen T. Schlachter, Bin Wang, Rui Xu, Hanbiao Yang, Xinlin Du, Guangzhou Han, Keshi Wang, Robert M. Czerwinski, Emily L. Ged, Heli Huang, Megan M. Halfmann, Melissa A. Maddie, Emily R. Morton, Sarah R. Olive, Huiling Tan, Shanhai Xie, John A. Josey, Eli M. Wallace

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Original Research

Direct syntheses of stereoisomers of 3-fluoro GABA and β-fluoroamine analogues of the calcium receptor (CaR) agonists, cinacalcet, tecalcet, fendiline and NPS R-467

Yohann J. G. Renault, Jiayin Diao, David B. Cordes, Katie Leach, David O’Hagan

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Many congratulations Nick!

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Mark Cockett

Chief Executive Officer | President of R&D | Head of Discovery | Oncology | Infectious Diseases | Site Leader | Team Leadership | R&D Strategy | Translational Medicine | Genomics | Small Molecules | Biologics

1 年

Great recognition for an impactful career! Well done Nick!!

Peter Bernstein

Owner PhaRmaB LLC

1 年

Congratulations Nick!

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Mick Hitchcock

Non Executive Chairman at Renogenyx (formerly EpiSwitch Rx)

1 年

Congratulations to you Nick - awesome career. Don't stop now ??

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Max Lataillade

Drug Development Expert | Visionary Leader in Antiviral Drug Discovery and Development | Physician-Researcher | Transforming Infectious Diseases and Global Health with Breakthrough Therapies

1 年

Congratulations Nick!

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