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Selective Inhibitors of Human Liver Carboxylesterase Based on a β-Lapachone Scaffold: Novel Reagents for Reaction Profiling

JOURNAL ARTICLE published 23 February 2017 in Journal of Medicinal Chemistry

Research funded by National Cancer Institute (CA108775,CA21765) | National Center for Complementary and Integrative Health (AT007531)

Authors: M. Jason Hatfield | Jingwen Chen | Ellie M. Fratt | Liying Chi | John C. Bollinger | Randall J. Binder | John Bowling | Janice L. Hyatt | Jerrod Scarborough | Cynthia Jeffries | Philip M. Potter

Design and Pharmacological Activity of Phosphinic Acid Based NAALADase Inhibitors

JOURNAL ARTICLE published 1 November 2001 in Journal of Medicinal Chemistry

Authors: Paul F. Jackson | Kevin L. Tays | Keith M. Maclin | Yao-Sen Ko | Weixing Li | Dil Vitharana | Takashi Tsukamoto | Doris Stoermer | Xi-Chun M. Lu | Krystyna Wozniak | Barbara S. Slusher

Solid-Phase Library Synthesis, Screening, and Selection of Tight-Binding Reduced Peptide Bond Inhibitors of a RecombinantLeishmaniamexicanaCysteine Protease B

JOURNAL ARTICLE published 1 May 2002 in Journal of Medicinal Chemistry

Authors: Phaedria M. St. Hilaire | Lira C. Alves | Fatima Herrera | Manat Renil | Sanya J. Sanderson | Jeremy C. Mottram | Graham H. Coombs | Maria A. Juliano | Luiz Juliano | Jorge Arevalo | Morten Meldal

Novel Cyclic Templates of α-MSH Give Highly Selective and Potent Antagonists/Agonists for Human Melanocortin-3/4 Receptors

JOURNAL ARTICLE published 1 June 2002 in Journal of Medicinal Chemistry

Authors: Malcolm J. Kavarana | Dev Trivedi | Minying Cai | Jinfa Ying | Matthew Hammer | Christopher Cabello | Paolo Grieco | Guoxia Han | Victor J. Hruby

Monocyclic Human Tachykinin NK-2 Receptor Antagonists as Evolution of a Potent Bicyclic Antagonist:  QSAR and Site-Directed Mutagenesis Studies

JOURNAL ARTICLE published 1 August 2002 in Journal of Medicinal Chemistry

Authors: Alessandro Giolitti | Maria Altamura | Francesca Bellucci | Danilo Giannotti | Stefania Meini | Riccardo Patacchini | Luigi Rotondaro | Sabrina Zappitelli | Carlo A. Maggi

Synthesis and in Vitro Evaluation of18F- and19F-Labeled Insulin:  A New Radiotracer for PET-based Molecular Imaging Studies

JOURNAL ARTICLE published 1 February 2006 in Journal of Medicinal Chemistry

Authors: Katharina J. Guenther | Sabesan Yoganathan | Robert Garofalo | Thomas Kawabata | Thomas Strack | Renée Labiris | Myrna Dolovich | Raman Chirakal | John F. Valliant

Procainamide–SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites

JOURNAL ARTICLE published 22 July 2021 in Journal of Medicinal Chemistry

Research funded by Pasteur Transversal Research Program (PTR 233-2019 HALBY) | Institut Carnot Institut Pasteur (S-CR18089-02B15 DARRI CONSO INNOV 46-19,S-PI15006-10A INNOV 05-2019 ARIMONDO IARP 2019-PC) | Agence national de Recherche (EpiKillMal)

Authors: Flore Nardella | Ludovic Halby | Irina Dobrescu | Johanna Viluma | Corentin Bon | Aurélie Claes | Véronique Cadet-Daniel | Ambre Tafit | Camille Roesch | Elie Hammam | Diane Erdmann | Melissa Mairet-Khedim | Roger Peronet | Salah Mecheri | Benoit Witkowski | Artur Scherf | Paola B. Arimondo

Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines:  Novel Non-Nucleoside Reverse Transcriptase Inhibitors of the S-DABO Series

JOURNAL ARTICLE published 1 May 1997 in Journal of Medicinal Chemistry

Authors: Antonello Mai | Marino Artico | Gianluca Sbardella | Silvana Quartarone | Silvio Massa | Anna G. Loi | Antonella De Montis | Franca Scintu | Monica Putzolu | Paolo La Colla

Novel Tetralone-Derived Retinoic Acid Metabolism Blocking Agents:  Synthesis and in Vitro Evaluation with Liver Microsomal and MCF-7 CYP26A1 Cell Assays

JOURNAL ARTICLE published 1 November 2005 in Journal of Medicinal Chemistry

Authors: Sook Wah Yee | Laetitia Jarno | Mohamed Sayed Gomaa | Carole Elford | Li-Ling Ooi | Michael P. Coogan | Richard McClelland | Robert Ian Nicholson | Bronwen A. J. Evans | Andrea Brancale | Claire Simons

Antitumor imidazotetrazines. 25. Crystal structure of 8-carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (temozolomide) and structural comparisons with the related drugs mitozolomide and DTIC

JOURNAL ARTICLE published September 1992 in Journal of Medicinal Chemistry

Authors: P. R. Lowe | C. E. Sansom | C. H. Schwalbe | M. F. G. Stevens | A. S. Clark

1,2,5-Thiadizole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists

JOURNAL ARTICLE published March 1982 in Journal of Medicinal Chemistry

Authors: Aldo A. Algieri | George M. Luke | Robert T. Standridge | Myron Brown | Richard A. Partyka | R. R. Crenshaw

5-(Haloalkyl)-2'-deoxyuridines: a novel type of potent antiviral nucleoside analog

JOURNAL ARTICLE published November 1985 in Journal of Medicinal Chemistry

Authors: Herfried Griengl | Michael Bodenteich | Walter Hayden | Erich Wanek | Wolfgang Streicher | Peter Stuetz | Helmut Bachmayer | Ismail Ghazzouli | Brigitte Rosenwirth

Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor

JOURNAL ARTICLE published 23 January 2020 in Journal of Medicinal Chemistry

Authors: Julien Lefranc | Volker Klaus Schulze | Roman Christian Hillig | Hans Briem | Florian Prinz | Anne Mengel | Tobias Heinrich | Jozsef Balint | Srinivasan Rengachari | Horst Irlbacher | Detlef Stöckigt | Ulf Bömer | Benjamin Bader | Stefan Nikolaus Gradl | Carl Friedrich Nising | Franz von Nussbaum | Dominik Mumberg | Daniel Panne | Antje Margret Wengner

5-C-Branched Deoxynojirimycin: Strategy for Designing a 1-Deoxynojirimycin-Based Pharmacological Chaperone with a Nanomolar Affinity for Pompe Disease

JOURNAL ARTICLE published 10 February 2022 in Journal of Medicinal Chemistry

Research funded by Japan Society for the Promotion of Science (JP21K06451) | National Natural Science Foundation of China (21272240)

Authors: Atsushi Kato | Izumi Nakagome | Uta Kanekiyo | Tian-Tian Lu | Yi-Xian Li | Kosuke Yoshimura | Mana Kishida | Kenta Shinzawa | Tomoki Yoshida | Nobutada Tanaka | Yue-Mei Jia | Robert J. Nash | George W. J. Fleet | Chu-Yi Yu

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

JOURNAL ARTICLE published 23 December 2021 in Journal of Medicinal Chemistry

Research funded by Norges Forskningsr??d (262613,267639) | Academy of Finland (287063,294085,319299) | South-Eastern Norway Regional Health Authority (15/00779-2,16/00528-9,2015012,2019090,2021035)

Authors: Ruben G. G. Leenders | Shoshy Alam Brinch | Sven T. Sowa | Enya Amundsen-Isaksen | Albert Galera-Prat | Sudarshan Murthy | Sjoerd Aertssen | Johannes N. Smits | Piotr Nieczypor | Eddy Damen | Anita Wegert | Marc Nazaré | Lari Lehtiö | Jo Waaler | Stefan Krauss

Synthesis and Cytotoxic Evaluation of Combretafurans, Potential Scaffolds for Dual-Action Antitumoral Agents

JOURNAL ARTICLE published 1 August 2006 in Journal of Medicinal Chemistry

Authors: Tracey Pirali | Sara Busacca | Lorena Beltrami | Daniela Imovilli | Francesca Pagliai | Gianluca Miglio | Alberto Massarotti | Luisella Verotta | Gian Cesare Tron | Giovanni Sorba | Armando A. Genazzani

Synthesis and Characterization of a Novel Gadolinium-Based Contrast Agent for Magnetic Resonance Imaging of Myelination

JOURNAL ARTICLE published 28 February 2013 in Journal of Medicinal Chemistry

Authors: Luca Frullano | Junqing Zhu | Robert H. Miller | Yanming Wang

Nitric Oxide Synthase Inhibitors That Interact with Both Heme Propionate and Tetrahydrobiopterin Show High Isoform Selectivity

JOURNAL ARTICLE published 22 May 2014 in Journal of Medicinal Chemistry

Research funded by National Institutes of Health (GM049725)

Authors: Soosung Kang | Wei Tang | Huiying Li | Georges Chreifi | Pavel Martásek | Linda J. Roman | Thomas L. Poulos | Richard B. Silverman

7-Deazaadenines Bearing Polar Substituents:  Structure−Activity Relationships of New A1 and A3 Adenosine Receptor Antagonists

JOURNAL ARTICLE published 1 November 2000 in Journal of Medicinal Chemistry

Authors: Sonja Hess | Christa E. Müller | Wolfram Frobenius | Ulrike Reith | Karl-Norbert Klotz | Kurt Eger

Application of the λ-Dynamics Method To Evaluate the Relative Binding Free Energies of Inhibitors to HCV Protease

JOURNAL ARTICLE published 1 December 2003 in Journal of Medicinal Chemistry

Authors: Zhuyan Guo | James Durkin | Thierry Fischmann | Richard Ingram | Andrew Prongay | Rumin Zhang | Vincent Madison