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Archive of "ACS Medicinal Chemistry Letters".

ISSN Print: 1948-5875

ISSN Online:

主页: https://www.ncbi.nlm.nih.gov/pmc/journals/2426/

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Atorvastatin (Lipitor) by MCR

Alexander D？mling,Constantinos G. Neochoritis,Tryfon Zarganes-Tzitzikas

Correction to “Light-Regulated NO Release as a Novel Strategy To Overcome Doxorubicin Multidrug Resistance”

Alberto Gasco,Aurore Fraix,Barbara Rolando,Chiara Riganti,Elena Gazzano,Gamal Eldein F. Abd-Ellatef,Konstantin Chegaev,Marco Blangetti,Roberta Fruttero,Sabrina Conoci,Salvatore Sortino

Behind the Mirror: Chirality Tunes the Reactivity and Cytotoxicity of Chloropiperidines as Potential Anticancer Agents

Alexander Francke,Alice Sosic,Barbara Gatto,Caterina Carraro,Daniele Fabris,Franziska Kohl,Michele De Franco,Richard G？ttlich,Tim Helbing

Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents

Addolorata Maria Luce Coluccia,Candice Gautier,Fiorella Di Pastena,Gianluca Canettieri,Giuseppe La Regina,Laura Di Magno,Maria Laura De Angelis,Marianna Nalli,Marta Baiocchi,Romano Silvestri,Stefano Biagioni,Stefano Gianni,Valentina Naccarato,Viviana Orlando

Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1)

Andrew Woodland,Claire Naylor,Colin Robinson,Daniel Fletcher,David Foley,Elad Katz,Erika Pinto,Gavin Wood,Jennifer Riley,Kevin D Read,Liam Ferguson,Lucy Ellis,Maria Osuna-Cabello,Ola Epemolu,Paul Scullion,Paul Wyatt,W. H. Irwin McLean,Yoko Shishikura

Synthesis, Biological Evaluation and Structure–Activity Relationships of Diflapolin Analogues as Dual sEH/FLAP Inhibitors

Abdulla Taha,Barbara Matuszczak,Christian Kretzer,Daniela Schuster,Erik Romp,Jana Fischer,Lisa Vieider,Martin Schoenthaler,Oliver Werz,Sonja Sturm,Veronika Temml,Victor Hernández-Olmos

Synthesis and Anti-HIV Profile of a Novel Tetrahydroindazolylbenzamide Derivative Obtained by Oxazolone Chemistry

Angela Scala,Anna Piperno,Frauke Christ,Nicola Micale,Zeger Debyser

High-Resolution Crystal Structure of Endoplasmic Reticulum Aminopeptidase 1 with Bound Phosphinic Transition-State Analogue Inhibitor

Margarete Neu,Paul Rowland,Petros Giastas

Correction to “Synthesis of 5-Thio-α-GalCer Analogues with Fluorinated Acyl Chain on Lipid Residue and Their Biological Evaluation”

Chuanfang Zhao,Jiao Lu,Min Fang,Peng He,Yang Zhang,Yuguo Du

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481

Arvind Mathur,Ashok Trehan,Catherine R. Burton,Charles F. Albright,Daniel Smith,Dmitry S. Zuev,James E. Grace,Jason M. Guernon,Jere E. Meredith,Jeremy H. Toyn,Jianliang Shi,Jianqing Li,John E. Macor,John S. Morrison,Kenneth M. Boy,Kimberley A. Lentz,Lawrence R. Marcin,Li Xu,Lorin A. Thompson,Mendi A. Higgins,Michael K. Ahlijanian,Rex Denton,Richard E. Olson,S. Roy Kimura,Subramaniam Krishnananthan,Tatyana Zvyaga,Xiaoliang Zhuo,Yong-Jin Wu,Yunhui Zhang

Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases

Albert Lai,Alexandre Nesterov,Arthur Kluge,Carmen Hertel,Ce Wang,David McElligott,Hong Liu,J. William Langston,John H. Van Drie,Kannan Karukurichi,Kenneth D. Bromberg,Loren Lasko,Michael Patane,Michael R. Michaelides,Peter de Vries,Philip A. Cole,Robert Mantei,Roberto M. Risi,Ronen Marmorstein,T. Matthew Hansen

Structure-Based Virtual Screening for the Discovery of Novel Inhibitors of New Delhi Metallo-β-lactamase-1

Donatella Tondi,Francesca Marcoccia,Francesca Spyrakis,Giuseppe Celenza,Laura Cendron,Mariagrazia Perilli,Matteo Santucci,Pierangelo Bellio,Simon Cross

Synthesis and Structure–Activity Relationship Study of Biliatresone, a Plant Isoflavonoid That Causes Biliary Atresia

Alyssa Kriegermeier,Jeffrey D. Winkler,Kristin Lorent,Michelle A. Estrada,Rebecca G. Wells,Seika A. Nagao,Simon Berritt,Xiao Zhao

Lysine Analogue of Polymyxin B as a Significant Opportunity for Photodynamic Antimicrobial Chemotherapy

Catherine Ouk,Emilie Pinault,Florent Le Guern,Regis Vanderesse,Tan-Sothea Ouk,Yves Champavier

Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors

Chunquan Sheng,Guoqiang Dong,Kun Fang,Shanchao Wu,Wei Wang,Ying Wu,Yu Li

Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy

Robert B. Kargbo

Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor

Chin-Ho Chen,Lan Xie,Lei Wei,Lei Zhu,Li Huang,Wei Li,Wei-Hong Lai

Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors

Caroline Hughes,Colin R. O’Dowd,Eamon Cassidy,Elias Arkoudis,Ewa Odrzywol,Ewelina Rozycka,Gerald Gavory,Hugues Miel,J. S. Shane Rountree,Jakub T. Flasz,Keeva McClelland,Linda Jordan,Matthew D. Helm,Natalie Page,Oliver Barker,Peter R. Hewitt,Scarlett Dvorkin,Stephanie Feutren-Burton,Timothy Harrison

Allosteric Modulators of Nicotinic Acetylcholine Receptors Useful for the Treatment of Cognitive Impairment

Benjamin E. Blass

Stereochemical Structure Activity Relationship Studies (S-SAR) of Tetrahydrolipstatin

George A. O’Doherty,Xiaofan Liu,Yanping Wang

Indolylmaleimide Derivative IM-17 Shows Cardioprotective Effects in Ischemia-Reperfusion Injury

Jun Sasamori,Katsuya Iuchi,Kazuyuki Aihara,Kosuke Dodo,Masahiro Takahashi,Naoki Terayama,Shuhei Nakao,Tadashi Shimizu

Click-Addressable Cassette for Photoaffinity Labeling

Bosheng Zhao,Kevin Burgess

Data Sets Representative of the Structures and Experimental Properties of FDA-Approved Drugs

Dominique Douguet

Water Solubility Enhancement of Pyrazolo[3,4-d]pyrimidine Derivatives via Miniaturized Polymer–Drug Microarrays

Ali Alazzo,Francesca Musumeci,Giovanna Sicilia,Jonathan C. Burley,Keith A. Spriggs,Martin C. Garnett,Monica Sanna,Nishant Singh,Silvia Schenone,Vincenzo Taresco

Using tert-Butyl Groups in a Ligand To Identify Its Binding Site on a Protein

Gottfried Otting,Wan-Na Chen

Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains

Brook M. Katzman,Chi S. Sum,Edgars Jecs,Eric J. Miller,Gretchen M. Schroeder,Huy H. Nguyen,Katie M. Kuo,Lawrence J. Wilson,Mary E. Cvijic,Michelle B. Kim,Robert J. Wilson,Tao Wang,Valarie M. Truax,Yesim A. Tahirovic

HTS by NMR for the Identification of Potent and Selective Inhibitors of Metalloenzymes

Carlo Baggio,Claudio Luchinat,Linda Cerofolini,Marco Fragai,Maurizio Pellecchia

18F-Radiolabeled Panobinostat Allows for Positron Emission Tomography Guided Delivery of a Histone Deacetylase Inhibitor

Benedict Law,Christopher S. Marnell,Harikrishna Kommidi,Hua Guo,Mark M. Souweidane,Richard Ting,Uday B. Maachani,Umberto Tosi

N-Leucinyl Benzenesulfonamides as Structurally Simplified Leucyl-tRNA Synthetase Inhibitors

Adéla？de Saint-Leger,Aigars Jirgensons,Alex J. O’Neill,Arya Gupta,Christopher P. Randall,Daina Gustina,Daina Lola,Einars Loza,Grace Edmund,Ilze Kaula,Kristaps Jaudzems,Lluís Ribas de Pouplana,Louise Kime,Marina Madre,Michael H. Charlton,Rihards Aleksis,Wil Goessens

Synthesis and Structure–Activity Relationships of Inhibitors That Target the C-Terminal MEEVD on Heat Shock Protein 90

Aldwin Guo,David A. Neale,Gabriel D. Moldovan,Gillian Thornton,Jenane Konesan,Jessica Kho,Laura K. Buckton,Lok K. O. Lam,Marwa N. Rahimi,Michael F. Lawler,Michael Leong,Samantha S. Zaiter,Shelli R. McAlpine,SuHyeon Kwon,Vickie Chan

The Attack of the Smart Particles: Should Bacteria Be Afraid?

Carina I. C. Crucho

Cell-Based Kinetic Target-Guided Synthesis of an Enzyme Inhibitor

Henrik Antti,Magnus Sellstedt

Amidate Prodrugs of Cyclic 9-(S)-[3-Hydroxy-2-(phosphonomethoxy)propyl]adenine with Potent Anti-Herpesvirus Activity

Elisabetta Groaz,Graciela Andrei,Min Luo,Piet Herdewijn,Robert Snoeck,Steven De Jonghe

Rhodanine as a Potent Scaffold for the Development of Broad-Spectrum Metallo-β-lactamase Inhibitors

Cheng Chen,Ke-Wu Yang,Li-Wei Xu,Peter Oelschlaeger,Wen-Ming Wang,Yang Xiang

Allosteric Modulation of Ionotropic Glutamate Receptors Special Issue

Nicholas I. Carruthers,Stephen F. Traynelis,Timothy W. Lovenberg

Azabicyclic Fused Pyrimidine Derivatives Useful for the Treatment of Alzheimer’s Disease

Benjamin E. Blass

2,7-Diazaspiro[4,4]nonanes for the Treatment or Prevention of Cancers and Diabetes

Robert B. Kargbo

BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder

Alicia Ng,Aliphedi B. Reddy,Arvind Mathur,Bettadapura N. Srikumar,Bradley C. Pearce,Charlie Albright,Charulatha Sanmathi,Dalton King,Eric Shields,G. Nagaraju,George N. Karageorge,Gopikishan Tonukunuru,Grandhi V. R. K. M. Gupta,Huiping Zhang,Hyunsoo Park,Imadul Islam,James Kempson,Jayakumar Warrier,Jayant Aher,Jean Simmermacher,Jianliang Shi,Jianqing Li,Joanne J. Bronson,John E. Macor,Jyoti Gulia,Kumar Kuchibhotla Vijaya,Lawrence R. Marcin,Linda J. Bristow,Lorin A. Thompson,Mahesh Paschapur,Manjunath Ramarao,Manjunatha Kamble,Michael Sinz,Michelle Nophsker,Murali Subramanian,Narasimharaju Kalidindi,Pattipati S. Naidu,Rajareddy Kallem,Raju Mannoori,Reeba Vikramadithyan,Rex Denton,Richard E. Olson,Srinivas Cheruku,Srinivas Jogi,Srinivasan Thangathirupathy,Tanmaya Bastia,Thaddeus Molski,Xiaoliang Zhuo

PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor

Alice Ye A. Chen,Christine S. Huang,David A. Gordon,David S. Taylor,Heather J. Finlay,James Neels,Ji Jiang,Joelle M. Onorato,Jon J. Hangeland,Lauren E. Haque,Leonard P. Adam,Lynn M. Abell,Michael D. Basso,Paul G. Sleph,R. Michael Lawrence,Richard Yang,Ruth R. Wexler,Thomas W. Harrity,Todd J. Friends,Xiaohong Yin

Correction to “Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure”

Mahesh S. Deshmukh,Nidhi Jain

Why Decreasing Lipophilicity Alone Is Often Not a Reliable Strategy for Extending IV Half-life

Fabio Broccatelli,Ignacio Aliagas

Chemical Proteomic Characterization of a Covalent KRASG12C Inhibitor

Aruna Wijeratne,Christopher Reutter,David A. Barda,John M. Strelow,Junpeng Xiao,Kelly W. Furness,Michael J. Chalmers,Mohammad Zia-Ebrahimi,Rachel N. Cavitt,Rebecca Leon,Robert D. Van Horn,Sheng-Bin Peng,Thomas A. Engler

Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling

Armand B. Cognetta, III,Benjamin F. Cravatt,Radu M. Suciu,Zachary E. Potter

Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET

Hai Yan,Michael R. Zalutsky,Satish K. Chitneni

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

Binghui Li,Cheryl H. Arrowsmith,Dalia Barsyte-Lovejoy,Ernesto Guccione,Fengling Li,Guillermo S. Cortez,Ken Weichert,Magdalena M. Szewczyk,Mary M. Mader,Masoud Vedadi,Michael J. Grogan,Mohammad S. Eram,Peter J. Brown,Robert M. Campbell,Stephen Antonysamy,Steven Kennedy,Wayne P. Bocchinfuso,Zahid Q. Bonday

MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

Charles D. Thompson,Christina N. Di Marco,Douglas C. Beshore,George D. Hartman,Joy Fuerst,Kenneth A. Koeplinger,Lei Ma,Marion Wittmann,Mark T. Bilodeau,Matthew A. Seager,Ronald K. Chang,Thomas J. Greshock,William J. Ray

3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus

Jin Soo Shin,Jinwoo Kim,Soo Bong Han,Sunjoo Ahn,Young-Sik Jung

Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor

Robert B. Kargbo

Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators

Armin Buschauer,Burkhard K？nig,Diana Pe？a-Solórzano,Günther Bernhardt,Matthias Scholler

Interpretation of in Vitro Metabolic Stability Studies for Racemic Mixtures

Iain J. Martin,James A. Baker,Michael D. Altman

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