medchem

Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A2B Adenosine Receptor Antagonists

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Ana Mallo-Abreu†‡, Rube´n Prieto-Di´az†‡, Willem Jespers§, Jhonny Azuaje†‡, Maria Majellaro†‡, Carmen Velando†, Xerardo Garci´a-Mera‡, Olga Caaman~o‡, Jose´ Brea*?, Mari´a I. Loza?, Hugo Gutie´rrez-de-Tera´n*§, and Eddy Sotelo*†‡
feedproxy.google.com/~r/acs/jmcmar/~3/1qU8NP1dGq8/acs.jmedchem.0c00564

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Mining Public Domain Data to Develop Selective DYRK1A Inhibitors

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Scott H. Henderson*†?, Fiona Sorrell#, James Bennett§, Marcus T. Hanley‡, Sean Robinson?, Iva Hopkins Navratilova??, Jonathan M. Elkins#?, and Simon E. Ward*‡
feedproxy.google.com/~r/acs/amclct/~3/EJtGSi6hNCU/acsmedchemlett.0c00279

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Discovery of Dihydropyrrolo[1,2-a]pyrazin-3(4H)-one-Based Second-Generation GluN2C- and GluN2D-Selective Positive Allosteric Modulators (PAMs) of the N-Methyl-d-Aspartate (NMDA) Receptor

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Matthew P. Epplin†, Ayush Mohan†, Lynnea D. Harris†, Zongjian Zhu‡, Katie L. Strong†, John Bacsa†, Phuong Le‡, David S. Menaldino†, Stephen F. Traynelis*‡, and Dennis C. Liotta*†
feedproxy.google.com/~r/acs/jmcmar/~3/14GwdcB2vm0/acs.jmedchem.9b01733

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Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Le Wang†, George A. Doherty†, Andrew S. Judd*†, Zhi-Fu Tao†, T. Matthew Hansen†, Robin R. Frey†, Xiaohong Song†, Milan Bruncko†, Aaron R. Kunzer†, Xilu Wang†, Michael D. Wendt†, John A. Flygare§#, Nathaniel D. Catron†, Russell A. Judge†, Chang H. Park†, Shashank Shekhar†, Darren C. Phillips†, Paul Nimmer†, Morey L. Smith†, Stephen K. Tahir†, Yu Xiao†, John Xue†, Haichao Zhang†, Phuong N. Le†, Michael J. Mitten†, Erwin R. Boghaert†, Wenqing Gao†, Peter Kovar†, Edna F. Choo§, Dolores Diaz§?, Wayne J. Fairbrother§, Steven W. Elmore†, Deepak Sampath§?, Joel D. Leverson†, and Andrew James Souers†
feedproxy.google.com/~r/acs/amclct/~3/c0aozCJa-Fw/acsmedchemlett.9b00568

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From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Kyler W. Pugh†§, Zheng Zhang†§, Jian Wang‡, Xiuzhi Xu‡, Vitumbiko Munthali†, Ang Zuo†, and Brian S. J. Blagg*†
feedproxy.google.com/~r/acs/amclct/~3/DvHL7HIJA3M/acsmedchemlett.0c00100

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Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein–Protein Inhibitors: Two Test Cases Illustrated by IL1ß-IL1R and p38a–TAB1 Complexes

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Charlie Nichols†‡, Joseph Ng‡, Annika Keshu‡, Geoff Kelly§, Maria R. Conte‡, Michael S. Marber†, Franca Fraternali‡, and Gian F. De Nicola*†‡
feedproxy.google.com/~r/acs/jmcmar/~3/tZv_V9eYnzg/acs.jmedchem.0c00403

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Structure–Permeability Relationship of Semipeptidic Macrocycles—Understanding and Optimizing Passive Permeability and Efflux Ratio

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Antoine Le Roux†, E´milie Blaise†, Pierre-Luc Boudreault†, Christian Comeau†, Annie Doucet†, Marilena Giarrusso†, Marie-Pierre Collin‡, Thomas Neubauer‡, Florian Ko¨lling‡, Andreas H. Go¨ller‡, Lea Seep‡, Dieudonne´ T. Tshitenge‡, Matthias Wittwer‡, Maximilian Kullmann‡, Alexander Hillisch‡, Joachim Mittendorf‡, and Eric Marsault*†
feedproxy.google.com/~r/acs/jmcmar/~3/d6fSGIb2fLI/acs.jmedchem.0c00013

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Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Yinuo Wu†, Yi-Jing Tian†, Mei-Ling Le†, Si-Rui Zhang, Chen Zhang, Meng-Xing Huang, Mei-Yan Jiang, Bei Zhang, and Hai-Bin Luo*
feedproxy.google.com/~r/acs/jmcmar/~3/qK0-jTXihy8/acs.jmedchem.0c00711

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Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Masakazu Atobe*†, Takayuki Serizawa†, Natsumi Yamakawa†#, Kenichiro Takaba†, Yukiko Nagano‡, Toshiaki Yamaura§, Eiichi Tanaka§, Atsutoshi Tazumi??, Shino Bito??, Masashi Ishiguro?, and Masashi Kawanishi†
feedproxy.google.com/~r/acs/jmcmar/~3/fJkqju23Wew/acs.jmedchem.0c00449

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Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Masakazu Atobe*†, Takayuki Serizawa†, Natsumi Yamakawa†#, Kenichiro Takaba†, Yukiko Nagano‡, Toshiaki Yamaura§, Eiichi Tanaka§, Atsutoshi Tazumi??, Shino Bito??, Masashi Ishiguro?, and Masashi Kawanishi†
feedproxy.google.com/~r/acs/jmcmar/~3/fJkqju23Wew/acs.jmedchem.0c00449

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Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Ulrich Lu¨cking*, Lars Wortmann*, Antje M. Wengner, Julien Lefranc, Philip Lienau, Hans Briem, Gerhard Siemeister, Ulf Bo¨mer, Karsten Denner, Martina Scha¨fer, Marcus Koppitz, Knut Eis, Florian Bartels, Benjamin Bader, Wilhelm Bone, Dieter Moosmayer, Simon J. Holton, Uwe Eberspa¨cher, Joanna Grudzinska-Goebel, Christoph Schatz, Gesa Deeg, Dominik Mumberg, and Franz von Nussbaum
feedproxy.google.com/~r/acs/jmcmar/~3/B9M1J_YSg7k/acs.jmedchem.0c00369

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Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Liu Hu†?, Xing Cai§?, Suzhen Dong§?, Yongjia Zhen†, Jidi Hu†, Shenjun Wang†, Jingwen Jiang†, Jiawu Huang†, Yuqiao Han§, Yu Qian*†‡, Yanqiu Yuan*†, and Wenhao Hu†‡
feedproxy.google.com/~r/acs/jmcmar/~3/gVn0SYaVCLs/acs.jmedchem.0c00079

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COVID-19: Drug Targets and Potential Treatments

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Carmen Gil*†, Tiziana Ginex†, Ine´s Maestro†, Vanesa Nozal†, Luci´a Barrado-Gil†, Miguel A´ngel Cuesta-Geijo†, Jesu´s Urquiza‡, David Rami´rez§, Covadonga Alonso‡, Nuria E. Campillo†, and Ana Martinez*†
feedproxy.google.com/~r/acs/jmcmar/~3/9VBcRkWJ2Os/acs.jmedchem.0c00606

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Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Liu Hu†?, Xing Cai§?, Suzhen Dong§?, Yongjia Zhen†, Jidi Hu†, Shenjun Wang†, Jingwen Jiang†, Jiawu Huang†, Yuqiao Han§, Yu Qian*†‡, Yanqiu Yuan*†, and Wenhao Hu†‡
feedproxy.google.com/~r/acs/jmcmar/~3/gVn0SYaVCLs/acs.jmedchem.0c00079

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Gadolinium-Based Neuroprognostic Magnetic Resonance Imaging Agents Suppress COX-2 for Prevention of Reperfusion Injury after Stroke

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Hee-Kyung Kim†‡, Jung-Jin Lee§, Garam Choi§?, Bokyung Sung?, Yeoun-Hee Kim§, Ah Rum Baek?, Soyeon Kim?, Huijin Song‡, Minsup Kim?, Art E. Cho?, Gang Ho Lee#, Sungjun Moon¶, Min-Kyoung Kang?, Jae Jun Lee?, and Yongmin Chang*???
feedproxy.google.com/~r/acs/jmcmar/~3/PEZr3AEFEmg/acs.jmedchem.0c00285

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Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Yongfu Liu†, Jun Wu†, Mingwei Zhou†, Wenming Chen†, Dongbo Li†, Zhanguo Wang†, Benoit Hornsperger?, Johannes D. Aebi?, Hans-Peter Ma¨rki?, Bernd Kuhn?, Lisha Wang‡, Andreas Kuglstatter#, Jo¨rg Benz#, Stephan Mu¨ller#, Remo Hochstrasser#, Giorgio Ottaviani?, Jian Xin§, Stephan Kirchner?, Susanne Mohr?, Philippe Verry?, William Riboulet?, Hong C. Shen†, Alexander V. Mayweg†?, Kurt Amrein?, and Xuefei Tan*†
feedproxy.google.com/~r/acs/jmcmar/~3/7tzP_x1IWF8/acs.jmedchem.0c00233

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Rapid Elaboration of Fragments into Leads by X-ray Crystallographic Screening of Parallel Chemical Libraries (REFiLX)

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Matthew R. Bentley†?, Olga V. Ilyichova†?, Geqing Wang‡, Martin L. Williams†, Gaurav Sharma†, Wesam S. Alwan†, Rebecca L. Whitehouse†, Biswaranjan Mohanty†#, Peter J. Scammells†, Begon~a Heras‡, Jennifer L. Martin§?, Makrina Totsika?, Ben Capuano†#, Bradley C. Doak*†#?, and Martin J. Scanlon*†#?
feedproxy.google.com/~r/acs/jmcmar/~3/ngQ4NvJr7uk/acs.jmedchem.0c00111

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Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Victoria C. Yan*†, Kristine L. Yang†, Elliot S. Ballato†, Sunada Khadka†, Prakriti Shrestha†‡, Kenisha Arthur†, Dimitra K. Georgiou†, Mykia Washington†, Theresa Tran†, Anton H. Poral†, Cong-Dat Pham†, Matthew J. Yan§, and Florian L. Muller*†
feedproxy.google.com/~r/acs/amclct/~3/TMk-kOvJbeY/acsmedchemlett.0c00203

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Rapid Elaboration of Fragments into Leads by X-ray Crystallographic Screening of Parallel Chemical Libraries (REFiLX)

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Matthew R. Bentley†?, Olga V. Ilyichova†?, Geqing Wang‡, Martin L. Williams†, Gaurav Sharma†, Wesam S. Alwan†, Rebecca L. Whitehouse†, Biswaranjan Mohanty†#, Peter J. Scammells†, Begon~a Heras‡, Jennifer L. Martin§?, Makrina Totsika?, Ben Capuano†#, Bradley C. Doak*†#?, and Martin J. Scanlon*†#?
feedproxy.google.com/~r/acs/jmcmar/~3/ngQ4NvJr7uk/acs.jmedchem.0c00111

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