Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Discovery of Novel UDP-<italic toggle="yes">N</italic>-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against <italic toggle="yes">Pseudomonas aeruginosa</italic>
  by M. Dominic Ryanα, Alastair L. Parkes, David Corbett, Anthony P. Dickie, Michelle Southey, Ole A. Andersen, Daniel B. Stein, Olivier R. Barbeau, Angelo Sanzone, Pia Thommes, John Barker, Ricky Cain, Christel Compper, Magali Dejob, Alain Dorali, Donnya Etheridge, Sian Evans, Adele Faulkner, Elise Gadouleau, Timothy Gorman, Denes Haase, Maisie Holbrow-Wilshaw, Thomas Krulle, Xianfu Li, Christopher Lumley, Barbara Mertins, Spencer Napier, Rajesh Odedra, Kostas Papadopoulos⋈, Vasileios Roumpelakis, Kate Spear, Emily Trimby⧓, Jennifer Williams, Michael Zahn⧖, Anthony D. Keefe, Ying Zhang, Holly T. Soutter◑, Paolo A. Centrella, Matthew A. Clark, John W. Cuozzo, Christoph E. Dumelin¤, Boer Deng☼, Avery Hunt◎, Eric A. Sigelα, Dawn M. Troast◐, and Boudewijn L. M. DeJonge
• [ASAP] Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold
  by Jian Rong, Wakana Mori, Xiaotian Xia, Michael A. Schafroth, Chunyu Zhao, Richard S. Van, Tomoteru Yamasaki, Jiahui Chen, Zhiwei Xiao, Ahmed Haider, Daisuke Ogasawara, Atsuto Hiraishi, Tuo Shao, Yiding Zhang, Zhen Chen, Fuwen Pang, Kuan Hu, Lin Xie, Masayuki Fujinaga, Katsushi Kumata, Yuancheng Gou, Yang Fang, Shuyin Gu, Huiyi Wei, Liang Bao, Hao Xu, Thomas L. Collier, Yihan Shao, Richard E. Carson, Benjamin F. Cravatt, Lu Wang, Ming-Rong Zhang, and Steven H. Liang
• [ASAP] Advances in the Therapeutic Application of Small-Molecule Inhibitors and Repurposed Drugs against Snakebite <subtitle>Miniperspective</subtitle>
  by Upasana Puzari, Pedro Alexandrino Fernandes, and Ashis K. Mukherjee
• [ASAP] Cinchona Alkaloid-Inspired Urea-Containing Autophagy Inhibitor Shows Single-Agent Anticancer Efficacy
  by Pei-Ru Jin, Yen-Nhi Ngoc Ta, I-Ting Chen, Yan-Ning Yu, Hsin Tzu Hsieh, Van-Anh Thi Nguyen, Shang-Ying Hsieh, Tiffaney Hsia, Hao Liu, Chan-Wei Hsu, Jeng-Liang Han, and Yunching Chen
• [ASAP] Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer
  by David M. Carter, Edgar Specker, Piotr H. Maecki, Jessica Przygodda, Krystyna Dudaniec, Manfred S. Weiss, Udo Heinemann, Marc Nazaré, and Ulrich Gohlke
• [ASAP] JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate
  by Frederik J. R. Rombouts, Ken-ichi Kusakabe, Richard Alexander, Nigel Austin, Herman Borghys, Michel De Cleyn, Deborah Dhuyvetter, Harrie J. M. Gijsen, Brian Hrupka, Tom Jacobs, Soufyan Jerhaoui, Lieve Lammens, Laurent Leclercq, Koichi Tsubone, Tatsuhiko Ueno, Kenji Morimoto, Shunsuke Einaru, Hirokazu Sumiyoshi, An Van den Bergh, Ann Vos, Michel Surkyn, Ard Teisman, and Diederik Moechars
• [ASAP] Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions
  by Tatsuhiko Ueno, Eriko Matsuoka, Naoya Asada, Shiho Yamamoto, Naoki Kanegawa, Mana Ito, Hisanori Ito, Diederik Moechars, Frederik J. R. Rombouts, Harrie J. M. Gijsen, and Ken-ichi Kusakabe
• [ASAP] Design, Synthesis, and Evaluation of Thienodiazepine Derivatives as Positron Emission Tomography Imaging Probes for Bromodomain and Extra-Terminal Domain Family Proteins
  by Ping Bai, Yu Lan, Debasis Patnaik, Hao Wang, Yan Liu, Zude Chen, Gengyang Yuan, Sepideh Afshar, Robin Striar, Julia S. Zagaroli, Darcy R. Tocci, Amelia G. Langan, Stephen J. Haggarty, and Changning Wang
• [ASAP] Synthesis and Anti-Influenza Virus Effects of Novel Substituted Polycyclic Pyridone Derivatives Modified from Baloxavir
  by Lin Tang, Haiyan Yan, Weibin Wu, Dawei Chen, Zhenxiong Gao, Jinqiang Hou, Cunlong Zhang, and Yuyang Jiang
• [ASAP] Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations
  by Zhijie Wang, Jiongheng Cai, Jiwei Ren, Yun Chen, Yingli Wu, Jie Cheng, Kun Jia, Fei Huang, Zitian Cheng, Tiancheng Sheng, Shiyu Song, Hao Heng, Yifan Zhu, Weifang Tang, Hongmei Li, Tao Lu, Yadong Chen, and Shuai Lu

ACS Medicinal Chemistry Letters

• [ASAP] Honokiol Prodrug Nanoparticles Based on In Situ Albumin Binding for Long Circulation and High Tumor Uptake
  by Lixue Chen, Shengnan Li, Yanfang Ding, Changyuan Wang, Sitong Zhang, Ruping Xu, Yali Chen, Hang Li, Meng Gao, Yan Qi, Youwei Xu, Xiaodong Ma, and Lei Li
• [ASAP] <italic toggle="yes">N</italic>-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors
  by Yangbo Feng, HaJeung Park, Jae Cheon Ryu, and Sung OK Yoon
• [ASAP] Novel HDAC1 and HDAC2 Inhibitors for Treating Diseases
  by Ram W. Sabnis
• [ASAP] Protein Degradation Inducers of Androgen Receptor by Conjugation of Antagonists Androgen Receptor and E3 Ligase Ligand
  by Robert B. Kargbo
• [ASAP] 2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors
  by Henri T. Pätsi, Tommi P. Kilpeläinen, Samuli Auno, Pyry M. J. Dillemuth, Khaled Arja, Maija K. Lahtela-Kakkonen, Timo T. Myöhänen, and Erik A. A. Wallén
• [ASAP] Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion
  by Brandon J. Kennedy, Ashley M. Lato, Alexander R. Fisch, Susan J. Burke, Justin K. Kirkland, Carson W. Prevatte, Lee E. Dunlap, Russell T. Smith, Konstantinos D. Vogiatzis, J. Jason Collier, and Shawn R. Campagna
• [ASAP] Modulation of KRAS Mutant by Inhibiting PLK1 Kinase in Cancer Therapeutics
  by Robert B. Kargbo
• [ASAP] Rational Design, Optimization, and Biological Evaluation of Novel MEK4 Inhibitors against Pancreatic Adenocarcinoma
  by Ada J. Kwong, Thao N. D. Pham, Hannah E. Oelschlager, Hidayatullah G. Munshi, and Karl A. Scheidt
• [ASAP] The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors
  by Wieslaw M. Kazmierski, Nagaraju Miriyala, David K. Johnson, and Sam Baskaran
• [ASAP] Novel Substituted Tetrahydroquinoline Compounds as Indoleamine-2,3-dioxygenase (IDO) Inhibitors
  by Ram W. Sabnis

Journal of Natural Products

• [ASAP] Voatriafricanines A and B, Trimeric Vobasine-Aspidosperma-Aspidosperma Alkaloids from <italic toggle="yes">Voacanga africana</italic>
  by Hugues Fouotsa, Pierre Le Pogam, Pierre Mkounga, Alain Meli Lannang, Guillaume Bernadat, Jérôme Vanheuverzwijn, Zhiyu Zhou, Karine Leblanc, Somia Rharrabti, Augustin Ephrem Nkengfack, Jean-François Gallard, Véronique Fontaine, Franck Meyer, Erwan Poupon, and Mehdi A. Beniddir
• [ASAP] Insights into Ergochromes of the Plant Pathogen <italic toggle="yes">Claviceps purpurea</italic>
  by Friederike Lünne, Jens Köhler, Christina Stroh, Lena Müller, Constantin G. Daniliuc, Christian Mück-Lichtenfeld∧, Ernst-Ulrich Würthwein∧, Melanie Esselen, Hans-Ulrich Humpf, and Svetlana A. Kalinina
• [ASAP] Withanolide-Type Steroids from <italic toggle="yes">Physalis nicandroides</italic> Inhibit HIV Transcription
  by Vito A. Taddeo, Marvin J. Núñez, Manuela Beltrán, Ulises G. Castillo, Jenny Menjívar, Ignacio A. Jiménez, José Alcamí, Luis M. Bedoya, and Isabel L. Bazzocchi
• [ASAP] Cudraflavone C from <italic toggle="yes">Artocarpus hirsutus</italic> as a Promising Inhibitor of Pathogenic, Multidrug-Resistant <italic toggle="yes">S. aureus</italic>, Persisters, and Biofilms: A New Insight into a Rational Explanation of Traditional Wisdom
  by Murugan Thulasi Meenu, Grace Kaul, Manjulika Shukla, Kokkuvayil Vasu Radhakrishnan, and Sidharth Chopra
• [ASAP] Biotransformation of Betulonic Acid by the Fungus <italic toggle="yes">Rhizopus arrhizus</italic> CGMCC 3.868 and Antineuroinflammatory Activity of the Biotransformation Products
  by Kai-Nan Song, You-Jia Lu, Cheng-Jiao Chu, Yan-Ni Wu, Hui-Lian Huang, Bo-Yi Fan, and Guang-Tong Chen
• [ASAP] Neuroregenerative Potential of Prenyl- and Pyranochalcones: A Structure–Activity Study
  by Corinna Urmann, Lara Bieler, Eleni Priglinger, Ludwig Aigner, Sebastien Couillard-Despres, and Herbert M. Riepl
• [ASAP] Direct Identification of α-Bisabolol Enantiomers in an Essential Oil Using a Combined Ion Mobility–Mass Spectrometry/Quantum Chemistry Approach
  by Erik Laurini, Stéphane Andreani, Alain Muselli, Sabrina Pricl, and Aura Tintaru