Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Searching for New Microbiome-Targeted Therapeutics through a Drug Repurposing Approach
  by Monica Barone, Simone Rampelli, Elena Biagi, Sine Mandrup Bertozzi, Federico Falchi, Andrea Cavalli, Andrea Armirotti, Patrizia Brigidi, Silvia Turroni, and Marco Candela
• [ASAP] Dual Cathepsin B and Glutathione-Activated Dimeric and Trimeric Phthalocyanine-Based Photodynamic Molecular Beacons for Targeted Photodynamic Therapy
  by Leo K. B. Tam, Ligang Yu, Roy C. H. Wong, Wing-Ping Fong, Dennis K. P. Ng, and Pui-Chi Lo
• [ASAP] New Insights into the Structure–Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of <bold>Neurounina-1</bold> as Modulators of the Na⁺/Ca²⁺ Exchanger Isoforms
  by Elisa Magli, Caterina Fattorusso, Marco Persico, Angela Corvino, Gianluca Esposito, Ferdinando Fiorino, Paolo Luciano, Elisa Perissutti, Vincenzo Santagada, Beatrice Severino, Valentina Tedeschi, Anna Pannaccione, Giuseppe Pignataro, Giuseppe Caliendo, Lucio Annunziato, Agnese Secondo, and Francesco Frecentese
• [ASAP] Synthetic Sansanmycin Analogues as Potent <italic toggle="yes">Mycobacterium tuberculosis</italic> Translocase I Inhibitors
  by Wendy Tran, Ali S. Kusay, Paige M. E. Hawkins, Chen-Yi Cheung, Gayathri Nagalingam, Venugopal Pujari, Daniel J. Ford, Alexander Stoye, Jessica L. Ochoa, Rebecca E. Audette, Elinor Hortle, Stefan H. Oehlers, Susan A. Charman, Roger G. Linington, Eric J. Rubin, Christopher G. Dowson, David I. Roper, Dean C. Crick, Thomas Balle, Gregory M. Cook, Warwick J. Britton, and Richard J. Payne
• [ASAP] Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket
  by Matthew G. Lloyd, Rosemary Huckvale, Kwai-Ming J. Cheung, Matthew J. Rodrigues, Gavin W. Collie, Olivier A. Pierrat, Mahad Gatti Iou, Michael Carter, Owen A. Davis, P. Craig McAndrew, Emma Gunnell, Yann-Vaï Le Bihan, Rachel Talbot, Alan T. Henley, Louise D. Johnson, Angela Hayes, Michael D. Bright, Florence I. Raynaud, Mirco Meniconi, Rosemary Burke, Rob L. M. van Montfort, Olivia W. Rossanese, Benjamin R. Bellenie, and Swen Hoelder
• [ASAP] Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of <italic toggle="yes">trans</italic>-4-<sc>l</sc>-Hydroxyprolyl-<sc>l</sc>-serine
  by Qikun Jiang, Qiuchi Xu, Yingli Wang, Pengyan Li, Yunran Zhang, Yongjun Wang, Jin Sun, Tianhong Zhang, and Zhonggui He
• [ASAP] First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53
  by Radosaw P. Nowak, Anthony Tumber, Eline Hendrix, Mohammad Salik Zeya Ansari, Manuela Sabatino, Lorenzo Antonini, Regina Andrijes, Eidarus Salah, Nicola Mautone, Francesca Romana Pellegrini, Klemensas Simelis, Akane Kawamura, Catrine Johansson, Daniela Passeri, Roberto Pellicciari, Alessia Ciogli, Donatella Del Bufalo, Rino Ragno, Mathew L. Coleman, Daniela Trisciuoglio, Antonello Mai, Udo Oppermann, Christopher J. Schofield, and Dante Rotili
• [ASAP] Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-<italic toggle="yes">N</italic>-(2′-methyl-3′-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1′-biphenyl]-4-yl)benzamide. Structure–Activity Relationship and Preclinical Characterization
  by Nilesh Raghunath Khedkar, Nageswara Rao Irlapatti, Disha Dadke, Vijay Kanoje, Zubair Shaikh, Vijay Karche, Vikas Shinde, Gokul Deshmukh, Amit Patil, Santosh Jachak, Samiron Phukan, Praveenkumar Anidil Kizhakinagath, Milind Gholve, Trupti Bhankhede, Jagadeesh Daler, Harshal Narendra Nemade, Sagar Budhe, Himani Pareek, Rajesh Yeshodharan, Rajesh Gupta, Anil Kalia, Dilip Pandey, Akshaya Wagh, Swaroop Kumar, Vinod Patil, Dipak Modi, Nidhi Sharma, Prajakta Ahirrao, Maneesh Mehta, Hemant Kumar, Prashant Nigade, Kaustubh Tamane, Sadanand Mallurwar, Sandip Kuldharan, Shashikant Pawar, Gururaj Vishwase, Sanjay Bokan, Minakshi Singh, Kumar Naik, Sachin Ingawale, Rajesh Shankar, Prabakaran Kamalakannan, Spinvin Venugopal, Shaji K. George, Kamlesh J. Padiya, Kumar V. S. Nemmani, Jaysagar Gundu, Mandar Bhonde, Lakshmi Narasimham, Milind Sindkhedkar, Chirag Shah, Neelima Sinha, Sharad Sharma, Dhananjay Bakhle, Rajender Kumar Kamboj, and Venkata P. Palle
• [ASAP] Relaxed Substrate Requirements of Sterol 14α-Demethylase from <italic toggle="yes">Naegleria fowleri</italic> Are Accompanied by Resistance to Inhibition
  by Tatiana Y. Hargrove, Zdzislaw Wawrzak, Girish Rachakonda, W. David Nes, Fernando Villalta, F. Peter Guengerich, and Galina I. Lepesheva
• [ASAP] Discovery of Novel Polycyclic Heterocyclic Derivatives from Evodiamine for the Potential Treatment of Triple-Negative Breast Cancer
  by Shengtao Xu, Hong Yao, Yangyi Qiu, Manzhen Zhou, Dahong Li, Liang Wu, Dong-Hua Yang, Zhe-Sheng Chen, and Jinyi Xu

ACS Medicinal Chemistry Letters

• [ASAP] Nanoparticular Inhibitors of Flavivirus Proteases from Zika, West Nile and Dengue Virus Are Cell-Permeable Antivirals
  by Barbara Schroeder, Peter Demirel, Christina Fischer, Enaam Masri, Stephanie Kallis, Lisa Redl, Thomas Rudolf, Silke Bergemann, Christoph Arkona, Christoph Nitsche, Ralf Bartenschlager, and Jörg Rademann
• [ASAP] Novel Heteroaromatic Carboxamide Derivatives as Plasma Kallikrein Inhibitors for Treating Diabetic Complications, Ocular Diseases and Edema-Associated Diseases
  by Ram W. Sabnis
• [ASAP] Novel Substituted Tetrazoles as ACSS2 Inhibitors for Treating Cancer
  by Ram W. Sabnis
• [ASAP] Novel Indole Compounds as TEAD Inhibitors for Treating Cancer
  by Ram W. Sabnis
• [ASAP] Ring Size as an Independent Variable in Cyclooligomeric Depsipeptide Antiarrhythmic Activity
  by Abigail N. Smith, Daniel J. Blackwell, Bjorn C. Knollmann, and Jeffrey N. Johnston
• [ASAP] Introducing the Tellurophene-Appended BODIPY: PDT Agent with Mass Cytometry Tracking Capabilities
  by Jacob W. Campbell, Matthew T. Tung, Roberto M. Diaz-Rodriguez, Katherine N. Robertson, Andrew A. Beharry, and Alison Thompson
• [ASAP] Adenosine Receptor Antagonists as Potential Cancer Therapy
  by Ahmed F. Abdel-Magid
• [ASAP] Dual Inhibition of IL-2-Inducible T-Cell Kinase (ITK) and Tropomyosin Receptor Kinase A (TRKA) as Potential Treatment for Atopic Dermatitis and Other Inflammatory and Autoimmune Diseases
  by Ahmed F. Abdel-Magid
• [ASAP] 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer
  by Emanuele M. Gargano△, Abdelrahman Mohamed△, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi▽, Hanna Drzewiecka, Pawe P. Jagodziński, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke□, Orazio Nicolotti▽, Angelo Carotti▽, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, and Martin Frotscher
• [ASAP] Novel Difluorocyclohexyl Derivatives as IL-17 Modulators for Treating Inflammatory and Autoimmune Diseases
  by Ram W. Sabnis

Journal of Natural Products

• [ASAP] Aureonitol Analogues and Orsellinic Acid Esters Isolated from <italic toggle="yes">Chaetomium elatum</italic> and Their Antineuroinflammatory Activity
  by Feng Ju, Qi-Xuan Kuang, Qing-Zhou Li, Li-Jun Huang, Wen-Xiu Guo, Lei-Qiang Gong, Yi-Fei Dai, Lun Wang, Yu-Cheng Gu, Dong Wang, Yun Deng, and Da-Le Guo
• [ASAP] Cytochalasin Derivatives from the Endozoic <italic toggle="yes">Curvularia verruculosa</italic> CS-129, a Fungus Isolated from the Deep-Sea Squat Lobster <italic toggle="yes">Shinkaia crosnieri</italic> Living in the Cold Seep Environment
  by Xue-Yi Hu, Chen-Yin Wang, Xiao-Ming Li, Sui-Qun Yang, Xin Li, Bin-Gui Wang&, Shu-Yi Si, and Ling-Hong Meng&
• [ASAP] Elucidation of the Streptoazine Biosynthetic Pathway in <italic toggle="yes">Streptomyces aurantiacus</italic> Reveals the Presence of a Promiscuous Prenyltransferase/Cyclase
  by Jing Liu, Yiling Yang, Lauritz Harken, and Shu-Ming Li
• [ASAP] Talarodrides A–F, Nonadrides from the Antarctic Sponge-Derived Fungus <italic toggle="yes">Talaromyces</italic> sp. HDN1820200
  by Yi Zhao, Chunxiao Sun, Luyao Huang, Xiao Zhang, Guojian Zhang, Qian Che, Dehai Li, and Tianjiao Zhu
• [ASAP] Correction to “The Berkeleylactones, Antibiotic Macrolides from Fungal Coculture”
  by Andrea A. Stierle, Donald B. Stierle, Daniel Decato, Nigel D. Priestley, Jeremy B. Alverson, John Hoody, Kelly McGrath, and Dorota Klepacki
• [ASAP] Artapilosines A and B, Unusual Phenanthrene Derivatives Related to Aporphine Alkaloids from <italic toggle="yes">Artabotrys pilosus</italic>
  by Yan-Ping Liu, Tong-Wei Wang, Zhen Xie, Yuan Bian, Yun-Yao Liu, Ruo-Qing Guan, Ze-Yu Liu, Lei Qiang, Guang-Ying Chen, and Yan-Hui Fu
• [ASAP] Irilone, a Red Clover Isoflavone, Combined with Progesterone Enhances PR Signaling through the Estrogen and Glucocorticoid Receptors
  by Julia R. Austin, Kailiang Li, Rocío Rivera Rodríguez, Daniel D. Lantvit, Brian T. Murphy, and Joanna E. Burdette
• [ASAP] Synthesis and Cytotoxic Activity of Lepidilines A–D: Comparison with Some 4,5-Diphenyl Analogues and Related Imidazole-2-thiones
  by Grzegorz Mlostoń, Mateusz Kowalczyk, Magorzata Celeda, Katarzyna Gach-Janczak, Anna Janecka, and Marcin Jasiński
• [ASAP] A Derivative of Piperlongumine and Ligustrazine as a Potential Thioredoxin Reductase Inhibitor in Drug-Resistant Hepatocellular Carcinoma
  by Jianqiang Qian, Zhongyuan Xu, Peng Zhu, Chi Meng, Yun Liu, Wenpei Shan, Ang He, Yipeng Gu, Fansheng Ran, Yanan Zhang, and Yong Ling
• [ASAP] Oxygenated Cyclohexene Derivatives from the Stem and Root Barks of <italic toggle="yes">Uvaria pandensis</italic>
  by Gasper Maeda, Pieter J. Gilissen, Anastasia Rudenko, Jelle van der Wal, Catarina Bourgard, Arvind Kumar Gupta, Per Sunnerhagen, Joan J. E. Munissi, Stephen S. Nyandoro, and Máté Erdélyi