Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Mechanistic Insights for Drug Repurposing and the Design of Hybrid Drugs for Alzheimer’s Disease
  by Dikshaa Padhi and Thimmaiah Govindaraju
• [ASAP] Discovery of Novel 7‑Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma
  by Zhenpeng Zhong, Liyang Shi, Tiancheng Fu, Jiajun Huang, and Zhengying Pan
• [ASAP] Palmatine Derivatives as Potential Antiplatelet Aggregation Agents via Protein Kinase G/Vasodilator-Stimulated Phosphoprotein and Phosphatidylinositol 3‑Kinase/Akt Phosphorylation
  by Tianyun Fan, Yangyang Cheng, Wei Wei, Qingxuan Zeng, Xixi Guo, Zhihao Guo, Yinghong Li, Liping Zhao, Yulong Shi, Xintong Zhang, Jiandong Jiang, Yanxiang Wang, Weijia Kong, and Danqing Song
• [ASAP] Penicillin Derivatives Inhibit the SARS-CoV‑2 Main Protease by Reaction with Its Nucleophilic Cysteine
  by Tika R. Malla, Lennart Brewitz, Dorian-Gabriel Muntean, Hiba Aslam, C. David Owen, Eidarus Salah, Anthony Tumber, Petra Lukacik, Claire Strain-Damerell, Halina Mikolajek, Martin A. Walsh, and Christopher J. Schofield
• [ASAP] Preventing Influenza A Virus Infection by Mixed Inhibition of Neuraminidase and Hemagglutinin by Divalent Inhibitors
  by Xuan Wei, Wenjuan Du, Margherita Duca, Guangyun Yu, Erik de Vries, Cornelis A. M. de Haan, and Roland J. Pieters
• [ASAP] Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein–Protein Interaction Inhibitors with an Alternative Binding Mode
  by Nikolaos Georgakopoulos, Sandeep Talapatra, Dina Dikovskaya, Sharadha Dayalan Naidu, Maureen Higgins, Jemma Gatliff, Aysel Ayhan, Roxani Nikoloudaki, Marjolein Schaap, Klara Valko, Farideh Javid, Albena T. Dinkova-Kostova, Frank Kozielski, and Geoffrey Wells
• [ASAP] Nontoxic Tumor-Targeting Optical Agents for Intraoperative Breast Tumor Imaging
  by Samer A. Naffouje, Masahide Goto, Lori U. Coward, Gregory S. Gorman, Konstantin Christov, Jing Wang, Albert Green, Anne Shilkaitis, Tapas K. Das Gupta, and Tohru Yamada
• [ASAP] Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases
  by Elisabetta Armani, Carmelida Capaldi, Valentina Bagnacani, Francesca Saccani, Giancarlo Aquino, Paola Puccini, Fabrizio Facchinetti, Cataldo Martucci, Nadia Moretto, Gino Villetti, Riccardo Patacchini, Maurizio Civelli, Chris Hurley, Andrew Jennings, Lilian Alcaraz, Dawn Bloomfield, Michael Briggs, Stephen Daly, Terry Panchal, Vince Russell, Sharon Wicks, Harry Finch, Mary Fitzgerald, Craig Fox, and Maurizio Delcanale
• [ASAP] Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease <italic toggle="yes">In Vivo</italic>
  by Yaoyao Yan, Chen Xing, Yun Xiao, Xiaobao Shen, Zhaoyan Zhang, Chuanbiao He, Jing-Bo Shi, Mingming Liu, and Xinhua Liu
• [ASAP] Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit
  by Nicky J. Willis, William Mahy, James Sipthorp, Yuguang Zhao, Hannah L. Woodward, Benjamin N. Atkinson, Elliott D. Bayle, Fredrik Svensson, Sarah Frew, Fiona Jeganathan, Amy Monaghan, Stefano Benvegnù, Sarah Jolly, Luca Vecchia, Reinis R. Ruza, Svend Kjær, Steven Howell, Ambrosius P. Snijders, Magda Bictash, Patricia C. Salinas, Jean-Paul Vincent, E. Yvonne Jones, Paul Whiting, and Paul V. Fish

ACS Medicinal Chemistry Letters

• [ASAP] Latest Research Trends in Agrochemical Fungicides: Any Learnings for Pharmaceutical Antifungals?
  by Clemens Lamberth
• [ASAP] Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy
  by Ram W. Sabnis
• [ASAP] Application of Rapidly Accelerating Fibrosarcoma Protein Degraders in Drug Discovery
  by Robert B. Kargbo
• [ASAP] Modified Benzofuran-carboxamide Compounds as Glucosylceramide Synthase Inhibitors for Treating Diseases
  by Ram W. Sabnis
• [ASAP] Novel Bis-phosphoglycerate Mutase Modulators for Treating Sickle Cell Disease
  by Ram W. Sabnis
• [ASAP] Targeting NOX2 via p47/phox-p22/phox Inhibition with Novel Triproline Mimetics
  by Jean-Baptiste Garsi, Balázs Komjáti, Gregorio Cullia, Imre Fejes, Melinda Sipos, Zoltán Sipos, Eszter Fördős, Piroska Markacz, Barbara Balázs, Nathalie Lancelot, Sylvie Berger, Eric Raimbaud, David Brown, Laurent-Michel Vuillard, Laure Haberkorn, Cyprian Cukier, Zoltán Szlávik, and Stephen Hanessian
• [ASAP] Antibacterial Nanoassembled Calix[4]arene Exposing Choline Units Inhibits Biofilm and Motility of Gram Negative Bacteria
  by Grazia Maria Letizia Consoli, Giuseppe Granata, Giovanna Ginestra, Andreana Marino, Giovanni Toscano, and Antonia Nostro
• [ASAP] Drug-like Inhibitors of DC-SIGN Based on a Quinolone Scaffold
  by Hengxi Zhang⊗, Ondřej Daněk, Dmytro Makarov, Stanislav Rádl, Dongyoon Kim⊗, Jiří Ledvinka, Kristýna Vychodilová, Jan Hlaváč, Jonathan Lefèbre⊗, Maxime Denis⊗, Christoph Rademacher⊗, and Petra Ménová
• [ASAP] Discovery and Preclinical Profiling of GSK3839919, a Potent HIV‑1 Allosteric Integrase Inhibitor
  by Kyle Parcella, Tao Wang, Kyle Eastman, Zhongxing Zhang, Zhiwei Yin, Manoj Patel, Yong Tu, Barbara Zhizhen Zheng, Michael A. Walker, Mark G. Saulnier, David Frennesson, Michael Bowsher, Eric Gillis, Kevin Peese, Makonen Belema, Christopher Cianci, Ira B. Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn D. Parker, Prasanna Sivaprakasam, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Susan Jenkins, John F. Kadow, Mark Krystal, Nicholas A. Meanwell, and B. Narasimhulu Naidu
• [ASAP] 1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum
  by Yanran Lu, Chelsea A. Mann, Sheri Nolan, Jessica A. Collins, Elizabeth Parker, Jonathan Papa, Sandip Vibhute, Seyedehameneh Jahanbakhsh, Mary Thwaites, David Hufnagel, Manzour H. Hazbón, Jane Moreno, Timothy T. Stedman, Thomas Wittum, Daniel J. Wozniak, Neil Osheroff, Jack C. Yalowich, and Mark J. Mitton-Fry

Journal of Natural Products

• [ASAP] Tanzawaic Acid Derivatives: Fungal Polyketides from the Deep-Sea Coral-Derived Endozoic <italic toggle="yes">Penicillium steckii</italic> AS-324
  by Xue-Yi Hu, Xiao-Ming Li, Bin-Gui Wang, and Ling-Hong Meng
• [ASAP] Isolation and Biosynthesis of Phenazine–Polyketide Hybrids from <italic toggle="yes">Streptomyces</italic> sp. KIB-H483
  by Zhiyan Wang, Feng-Xian Yang, Chongxi Liu, Li Wang, Yuxin Qi, Minghang Cao, Xiaowei Guo, Jie Li, Xueshuang Huang, Jing Yang, and Sheng-Xiong Huang
• [ASAP] Calysepins I–VII, Hexasaccharide Resin Glycosides from <italic toggle="yes">Calystegia sepium</italic> and Their Cytotoxic Evaluation
  by Kai-Qing Lv, Hong-Ying Ji, Gao-Xiang Du, Shou Peng, Peng-Ju Guo, Ge Wang, Yao Zhu, Qing Wang, Wen-Qiong Wang, and Li-Jiang Xuan
• [ASAP] Tuaimenal A, a Meroterpene from the Irish Deep-Sea Soft Coral <italic toggle="yes">Duva florida</italic>, Displays Inhibition of the SARS-CoV‑2 3CLpro Enzyme
  by Nicole E. Avalon, Jordan Nafie, Carolina De Marco Verissimo, Luke C. Warrensford, Sarah G. Dietrick, Amanda R. Pittman, Ryan M. Young, Fiona L. Kearns△, Tracess Smalley□, Jennifer M. Binning□, John P. Dalton, Mark P. Johnson, H. Lee Woodcock, A. Louise Allcock, and Bill J. Baker
• [ASAP] Antitumor Activity of Rutaecarpine in Human Colorectal Cancer Cells by Suppression of Wnt/β-Catenin Signaling
  by Woong Sub Byun, Eun Seo Bae, Won Kyung Kim, and Sang Kook Lee
• [ASAP] Hernandezine Regulates Proliferation and Autophagy-Induced Apoptosis in Melanoma Cells
  by Xiaoting Wang, Xiaojie Li, Yuan Xia, Danyang Wang, Xiaohan Li, Ling Liu, Qiusheng Zheng, Defang Li, and Qingling Jiang
• [ASAP] Design and Synthesis of Novel Celastrol Derivatives as Potential Anticancer Agents against Gastric Cancer Cells
  by Zhi-Chao Lei, Na Li, Nai-Rong Yu, Wei Ju, Xiao-Na Sun, Xue-Ling Zhang, Hai-Juan Dong, Jian-Bo Sun, and Li Chen
• [ASAP] Ansellone J, a Potent <italic toggle="yes">in Vitro</italic> and <italic toggle="yes">ex Vivo</italic> HIV‑1 Latency Reversal Agent Isolated from a <italic toggle="yes">Phorbas</italic> sp. Marine Sponge
  by Meng Wang, Amanda Sciorillo, Silven Read, Donya Naz Divsalar, Kwasi Gyampoh, Guorui Zu, Zhe Yuan, Karam Mounzer□, David E. Williams, Luis J. Montaner, Nicole de Voogd, Ian Tietjen, and Raymond J. Andersen
• [ASAP] Spirocitromycetin, a Fungal Polyketide with an Antiosteoporotic Pharmacophore
  by Yong Chen, Ying Jie Wei, Nan Jiang, Hui Ming Ge, Rui Hua Jiao, Xu Cheng, and Ren Xiang Tan
• [ASAP] Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived <italic toggle="yes">Streptomyces</italic>
  by Kantinan Leetanasaksakul, Wilaiwan Koomsiri, Takuya Suga, Hirotaka Matsuo, Rei Hokari, Pakorn Wattana-Amorn, Yo̅ko Takahashi, Kazuro Shiomi, Takuji Nakashima, Yuki Inahashi, and Arinthip Thamchaipenet