ChemMedChem

Cover image for Vol. 9 Issue 12

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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December 18, 2014

The Year in (Mini)Review!

The Year in (Mini)Review!ChemMedChem Volume 9 saw a great number of high-quality secondary publications. The four special issues published in 2014 hosted some particularly insightful Review and Minireview articles written by experts in their fields. All reviews published in ChemMedChem are meant to provide concise yet comprehensive summaries and analysis of recent developments within a given subtopic of medicinal chemistry, which should benefit both seasoned researchers as well as scientists just starting their careers. Read more...

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December 18, 2014

The Year in (Mini)Review!

The Year in (Mini)Review!ChemMedChem Volume 9 saw a great number of high-quality secondary publications. The four special issues published in 2014 hosted some particularly insightful Review and Minireview articles written by experts in their fields. All reviews published in ChemMedChem are meant to provide concise yet comprehensive summaries and analysis of recent developments within a given subtopic of medicinal chemistry, which should benefit both seasoned researchers as well as scientists just starting their careers. Therefore, to wrap up 2014, we thought we would compile a list of all Reviews and Minireviews published over the past year; happy reading! And don't forget: all articles in Issue 01 are free to access.

M. Kyle Hadden, Hedgehog Pathway Agonism: Therapeutic Potential and Small-Molecule Development (issue 01 (free access!), pages 27–37)

Prof. Marcello Leopoldo, Dr. Marialessandra Contino, Prof. Francesco Berardi, Prof. Roberto Perrone and Prof. Nicola Antonio Colabufo, PET Radiotracers for Imaging P-glycoprotein: The Challenge for Early Diagnosis in AD (issue 01 (free access!), pages 38–42)

Dr. Stephen P. Andrews, Dr. Giles A. Brown and Dr. John A. Christopher, Structure-Based and Fragment-Based GPCR Drug Discovery (issue 02, pages 256–275)

Dr. Daniel Gallenkamp, Dr. Kathy A. Gelato, Dr. Bernard Haendler and Dr. Hilmar Weinmann, Bromodomains and Their Pharmacological Inhibitors (issue 03 (Epigenetics & Drug Discovery special issue), pages 438–464)

Tobias Wagner, Dr. Dina Robaa, Prof. Dr. Wolfgang Sippl and Prof. Dr. Manfred Jung, Mind the Methyl: Methyllysine Binding Proteins in Epigenetic Regulation (issue 03 (Epigenetics & Drug Discovery special issue), pages 466–483)

Nadeem A. Vellore and Prof. Riccardo Baron, Epigenetic Molecular Recognition: A Biomolecular Modeling Perspective (issue 03 (Epigenetics & Drug Discovery special issue), pages 484–494)

Beat Fierz, Synthetic Chromatin Approaches To Probe the Writing and Erasing of Histone Modifications (issue 03 (Epigenetics & Drug Discovery special issue), pages 495–504)

Dr. Mariangela Morlando, Dr. Monica Ballarino, Prof. Alessandro Fatica and Prof. Irene Bozzoni, The Role of Long Noncoding RNAs in the Epigenetic Control of Gene Expression (issue 03 (Epigenetics & Drug Discovery special issue), pages 505–510)

Prof. Michael W. Van Dyke, Lysine Deacetylase (KDAC) Regulatory Pathways: an Alternative Approach to Selective Modulation (issue 03 (Epigenetics & Drug Discovery special issue), pages 511–522)

Dr. Florian Thaler and Dr. Ciro Mercurio, Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next (issue 03 (Epigenetics & Drug Discovery special issue), pages 523–536)

Fatima Ismail and Prof. David A. Winkler, Getting to the Source: Selective Drug Targeting of Cancer Stem Cells (issue 05 (AIMECS special issue), pages 885–898)

Sulin Zhang, Prof. Yanling Wu and Prof. Wen Zhang, G-Quadruplex Structures and Their Interaction Diversity with Ligands (issue 05 (AIMECS special issue), pages 899–911)

Johannes Notni, Jakub Simecek and Hans-Jürgen Wester, Phosphinic Acid Functionalized Polyazacycloalkane Chelators for Radiodiagnostics and Radiotherapeutics: Unique Characteristics and Applications (issue 06 (Metals in Medicine special issue), pages 1107–1115)

Quyen N. Do, Dr. James S. Ratnakar, Dr. Zoltán Kovács and Prof. A. Dean Sherry, Redox- and Hypoxia-Responsive MRI Contrast Agents (issue 06 (Metals in Medicine special issue), pages 1116–1129)

Dr. F. Ivy Carroll and Dr. Roland E. Dolle, The Discovery and Development of the N-Substituted trans-3,4-Dimethyl-4-(3′-hydroxyphenyl)piperidine Class of Pure Opioid Receptor Antagonists (issue 08, pages 1638–1654)

Arunoday Bhan and Prof. Subhrangsu S. Mandal, Long Noncoding RNAs: Emerging Stars in Gene Regulation, Epigenetics and Human Disease (issue 09 (DNA & RNA Med. Chem. special issue), pages 1932–1956)

Dr. Akimitsu Okamoto, DNA–Osmium Complexes: Recent Developments in the Operative Chemical Analysis of DNA Epigenetic Modifications (issue 09 (DNA & RNA Med. Chem. special issue), pages 1958–1965)

Dr. Attilio V. Vargiu and Dr. Alessandra Magistrato, Atomistic-Level Portrayal of Drug–DNA Interplay: A History of Courtships and Meetings Revealed by Molecular Simulations (issue 09 (DNA & RNA Med. Chem. special issue), pages 1966–1981)

Aurélie Blond, Dr. Eric Ennifar, Dr. Carine Tisné and Dr. Laurent Micouin, The Design of RNA Binders: Targeting the HIV Replication Cycle as a Case Study (issue 09 (DNA & RNA Med. Chem. special issue), pages 1982–1996)

Sven Kruspe, Florian Mittelberger, Kristina Szameit and Prof. Dr. Ulrich Hahn, Aptamers as Drug Delivery Vehicles (issue 09 (DNA & RNA Med. Chem. special issue), pages 1998–2011)

Pengfei Zhan, Qiao Jiang, Prof. Zhen-gang Wang, Na Li, Prof. Haiyin Yu and Prof. Baoquan Ding, DNA Nanostructure-Based Imaging Probes and Drug Carriers (issue 09 (DNA & RNA Med. Chem. special issue), pages 2013–2020)

Ravi Naik, Dr. Brice W. Obiang-Obounou, Minkyoung Kim, Prof. Yongseok Choi, Dr. Hyun Sun Lee and Prof. Kyeong Lee, Therapeutic Strategies for Metabolic Diseases: Small-Molecule Diacylglycerol Acyltransferase (DGAT) Inhibitors (issue 11, pages 2410–2424)

Can Zhao and Prof. Shutao Ma, Recent Advances in The Discovery of N-Myristoyltransferase Inhibitors (issue 11, pages 2425–2437)

Dr. Giovanni M. Pavan, Modeling the Interaction between Dendrimers and Nucleic Acids: a Molecular Perspective through Hierarchical Scales (issue 12, pages 2623–2631)

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December 07, 2014

Research that Never Sleeps

Research that Never SleepsYves P. Auberson and colleagues at Novartis Institutes for BioMedical Research (NIBR), in collaboration with scientists at ChemPartner (Shanghai, China), made a big splash last August with their ChemMedChem issue cover and Full Paper, Ergoline-Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy. Read the Sleep Solutions article in the NIBR newsroom for a synopsis!

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December 01, 2014

Excellence with ChemXChem Journals

Excellence with ChemXChem JournalsChemMedChem and its series of ChemXChem sister journals have enjoyed enormous success! To highlight a sample of content across the series, more than 20 of the best articles are now free to read until the end of February 2015. Check out the article in ChemistryViews for links to these articles as well as an Editorial that summarizes current happenings and near-future plans for each journal.

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November 22, 2014

The Most Accessed Are More Accessible

The Most Accessed Are More AccessibleChemMedChem's top-24 most-accessed articles of the last 12 months are now free to access! The diverse topics covered by these articles reflect the broad scope of the journal; we hope you find them as engaging as we do. Happy reading!

Lluís Ballell et al., Fueling Open-Source Drug Discovery: 177 Small-Molecule Leads against Tuberculosis

Stefan Peukert, Karen Miller-Moslin, Small-Molecule Inhibitors of the Hedgehog Signaling Pathway as Cancer Therapeutics

Zhengying Pan et al., Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase

Felix Kratz et al., Prodrug Strategies in Anticancer Chemotherapy

Carlo Ballatore et al., Carboxylic Acid (Bio)Isosteres in Drug Design

Yijing Li et al., Thiadiazole–a Promising Structure in Medicinal Chemistry

Daniel Gallenkamp et al., Bromodomains and Their Pharmacological Inhibitors

Martin Morgenthaler et al., Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities

Thomas W. Bell, Drugs for Hepatitis C: Unlocking a New Mechanism of Action

Ruth Brenk et al., Lessons Learnt from Assembling Screening Libraries for Drug Discovery for Neglected Diseases

Jeremy Murray et al., Tailoring Small Molecules for an Allosteric Site on Procaspase-6

Tian-miao Ou et al., G-Quadruplexes: Targets in Anticancer Drug Design

Edmond Differding, Drug Discovery Alliances in India–Indications, Targets, and New Chemical Entities

Edgar Jacoby et al., The 7 TM G-Protein-Coupled Receptor Target Family

M. Kyle Hadden, Hedgehog Pathway Agonism: Therapeutic Potential and Small-Molecule Development

L. W. Lawrence Woo et al., Structure–Activity Relationship for the First-in-Class Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495)

Antonello Mai, Targeting Epigenetics in Drug Discovery

Alexander Böcker et al., Development of Specific "Drug-Like Property" Rules for Carboxylate-Containing Oral Drug Candidates

Daniel Spinks et al., Design, Synthesis and Biological Evaluation of Trypanosoma brucei Trypanothione Synthetase Inhibitors

Ahmed Kamal et al., Synthesis and Biological Evaluation of Benzo[b]furans as Inhibitors of Tubulin Polymerization and Inducers of Apoptosis

Elizabeth I. Parkinson, Paul J. Hergenrother, Runaway ROS as a Selective Anticancer Strategy

Steven R. LaPlante et al., Revealing Atropisomer Axial Chirality in Drug Discovery

Stephen P. Andrews et al., Structure-Based and Fragment-Based GPCR Drug Discovery

Astrid Spannhoff et al., The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors

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November 22, 2014

The Most Accessed Are More Accessible

The Most Accessed Are More AccessibleChemMedChem's top-24 most-accessed articles of the last 12 months are now free to access! The diverse topics covered by these articles reflect the broad scope of the journal. Read more...

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November 04, 2014

VIP: Design of gem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological Evaluation

VIP: Design of gem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological EvaluationHIV-1 protease plays a critical role in replication of the human immunodeficiency virus (HIV). Compounds that inhibit HIV-1 protease are an important component of combined antiretroviral therapy. Current antiretroviral therapy has significantly decreased morbidity and mortality in HIV/AIDS patients. However, there are growing concerns regarding the long-term suppression of virus replication with current therapies, given the development of drug-resistant HIV strains, as well as neurological complications. The central nervous system (CNS) can serve as a reservoir for HIV-1 infection. HIV-associated dementia and other CNS disorders are increasing due to poor CNS penetration of current anti-HIV therapies.

A collaborative research effort by Arun Ghosh and colleagues at Purdue University and Hiroaki Mitsuya and colleagues at the National Cancer Institute and Kumamoto School of Medicine, has led to the design of specific fluorine-containing HIV-1 protease inhibitors based on their previous FDA-approved drug, darunavir. These structural changes resulted in significantly improved brain penetration of the drug and potently inhibited multidrug-resistant HIV. Furthermore, X-ray structural studies in collaboration with Irene Weber and colleagues at the University of Georgia confirmed that these fluorine-containing drugs make extensive binding interactions in the enzyme active site, including hydrogen bonding with the HIV-1 protease backbone and an interesting fluorine–carbonyl oxygen non-bonding interaction in the S2 sub-pocket. These interactions are consistent with the “backbone binding” concept in drug design that they have put forward to develop therapies with improved drug resistance properties.

Received August 18, 2014; published online October 21, 2014, DOI: 10.1002/cmdc.201402358.

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October 29, 2014

Free to Read!

Free to Read!Did you know that some of the best articles in ChemMedChem are free to read throughout the year? Just look for the gold (free to read for a limited time) or purple (open access article) open-lock logos online in EarlyView or within an Issue.

The purple lock indicates that the author has made use of our OnlineOpen service, in which the article is published open access under a Creative Commons license. More information is given at www.chemmedchem.org/open.

The January issue is free to read throughout the year: Issue 01/2014 is currently free to read; this and other issues can be accessed through the journal's homepage.

Register on Wiley Online Library and sign up for subject-based newsletters to stay up to date on ChemMedChem and related Wiley journals and books. Fan of the journal? Follow us on Twitter, like us on Facebook, sign up for eToC or EarlyView alerts, or get the RSS feed—there have never been more ways to stay up to date on your favorite content!

Articles currently free to read:

R. Buratto et al., Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR. ChemMedChem 2014, 9, 2509–2515; DOI: 10.1002/cmdc.201402214 [OnlineOpen]

A. R. Mandhapati et al., Importance of the 6'-Hydroxy Group and Its Configuration for Apramycin Activity. ChemMedChem 2014, 9, 2074–2083; DOI: 10.1002/cmdc.201402146

E. Barile et al., Design, Synthesis and Bioevaluation of an EphA2 Receptor-Based Targeted Delivery System. ChemMedChem 2014, 9, 1403–1412; DOI: 10.1002/cmdc.201400067

F. Rechenmacher et al., The Integrin Ligand c(RGDf(NMe)Nal) Reduces Neointimal Hyperplasia in a Polymer-Free Drug-Eluting Stent System. ChemMedChem 2014, 9, 1413–1418; DOI: 10.1002/cmdc.201400078

M. P. Leese et al., Synthesis, Anti-tubulin and Antiproliferative SAR of Steroidomimetic Dihydroisoquinolinones. ChemMedChem 2014, 9, 798–812; DOI: 10.1002/cmdc.201400017 [OnlineOpen]

S. M. Saalau-Bethell et al., Crystal Structure of Human Soluble Adenylate Cyclase Reveals a Distinct, Highly Flexible Allosteric Bicarbonate Binding Pocket. ChemMedChem 2014, 9, 823–832; DOI: 10.1002/cmdc.201300480 [OnlineOpen]

C. A. Olsen, An Update on Lysine Deacylases Targeting the Expanding “Acylome”. ChemMedChem 2014, 9, 434–437; DOI: 10.1002/cmdc.201300421

D. Gallenkamp et al., Bromodomains and Their Pharmacological Inhibitors. ChemMedChem 2014, 9, 438–464; DOI: 10.1002/cmdc.201300434

E. Rilova et al., Design, Synthesis and Biological Evaluation of 4-Amino-N-(4-aminophenyl)benzamide Analogues of Quinoline-Based SGI-1027 as Inhibitors of DNA Methylation. ChemMedChem 2014, 9, 590–601; DOI: 10.1002/cmdc.201300420 [OnlineOpen]

A. S. Madsen et al., The Effect of Various Zinc Binding Groups on Inhibition of Histone Deacetylases 1–11. ChemMedChem 2014, 9, 614–626; DOI: 10.1002/cmdc.201300433

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December 18, 2014
The Year in (Mini)Review!

December 18, 2014
The Year in (Mini)Review!

December 07, 2014
Research that Never Sleeps

December 01, 2014
Excellence with ChemXChem Journals

November 22, 2014
The Most Accessed Are More Accessible

November 22, 2014
The Most Accessed Are More Accessible

November 04, 2014
VIP: Design of gem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological Evaluation

October 29, 2014
Free to Read!

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