Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer
  by Matthew J. LaMarche, Michael Acker, Andreea Argintaru, Daniel Bauer, Julie Boisclair, Homan Chan, Christine Hiu-Tung Chen, Ying-Nan Chen, Zhouliang Chen, Zhan Deng, Michael Dore, David Dunstan, Jianmei Fan, Peter Fekkes, Brant Firestone, Michelle Fodor, Jorge Garcia-Fortanet, Pascal D. Fortin, Cary Fridrich, John Giraldes, Meir Glick, Denise Grunenfelder, Huia-Xiang Hao, Martin Hentemann, Samuel Ho, Andriana Jouk, Zhao B. Kang, Rajesh Karki, Mitsunori Kato, Nick Keen, Robert Koenig, Laura R. LaBonte, Jay Larrow, Gang Liu, Shumei Liu, Dyuti Majumdar, Simon Mathieu, Matthew J. Meyer, Morvarid Mohseni, Rukundo Ntaganda, Mark Palermo, Lawrence Perez, Minying Pu, Timothy Ramsey, John Reilly, Patrick Sarver, William R. Sellers, Martin Sendzik, Michael D. Shultz, Joanna Slisz, Kelly Slocum, Troy Smith, Stanley Spence, Travis Stams, Christopher Straub, Victoriano Tamez, Jr., Bakary-Barry Toure, Christopher Towler, Ping Wang, Hongyun Wang, Sarah L. Williams, Fan Yang, Bing Yu, Ji-Hu Zhang, and Suzanne Zhu
• [ASAP] Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers
  by Chaoguo Cao, Jie Yang, Yong Chen, Peiting Zhou, Yingwei Wang, Wu Du, Lifeng Zhao, and Yuanwei Chen
• [ASAP] Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1–13)-NH₂
  by Salvatore Pacifico, Federica Ferrari, Valentina Albanese, Erika Marzola, Joaquim Azevedo Neto, Chiara Ruzza, Girolamo Calò, Delia Preti, and Remo Guerrini
• [ASAP] Development of Bis-cyclic Imidazolidine-4-one Derivatives as Potent Antibacterial Agents
  by Minghui Wang, Ruixuan Gao, Mengmeng Zheng, Peng Sang, Chunpu Li, En Zhang, Qi Li, and Jianfeng Cai
• [ASAP] Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3Kα and mTOR Kinases for the Treatment of Solid Tumors
  by Dinesh Mahajan, Somdutta Sen, Bilash Kuila, Amit Sharma, Reena Arora, Milind Sagar, Amal Ray Mahapatra, Lalita Babasaheb Gawade, and Sundeep Dugar
• [ASAP] Therapeutic Exploitation of GPR18: Beyond the Cannabinoids? <subtitle>Miniperspective</subtitle>
  by Paula Morales, Ana Lago-Fernandez, Dow P. Hurst, Noori Sotudeh, Eugen Brailoiu, Patricia H. Reggio, Mary E. Abood, and Nadine Jagerovic
• [ASAP] Discovery of 9-Cyclopropylethynyl-2-((<italic toggle="yes">S</italic>)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-<italic toggle="yes">a</italic>]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial
  by Frédéric Labéguère, Sonia Dupont, Luke Alvey, Florilène Soulas, Gregory Newsome, Amynata Tirera, Vanessa Quenehen, Thi Thu Trang Mai, Pierre Deprez, Roland Blanqué, Line Oste, Sandrine Le Tallec, Steve De Vos, Annick Hagers, Ann Vandevelde, Luc Nelles, Nele Vandervoort, Katja Conrath, Thierry Christophe, Ellen van der Aar, Emanuelle Wakselman, Didier Merciris, Céline Cottereaux, Cécile da Costa, Laurent Saniere, Philippe Clement-Lacroix, Laura Jenkins, Graeme Milligan, Stephen Fletcher, Reginald Brys, and Romain Gosmini
• [ASAP] Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies
  by Simon Gonzalez, Maria Dumitrascuta, Emilie Eiselt, Stevany Louis, Linda Kunze, Annalisa Blasiol, Mélanie Vivancos, Santo Previti, Elke Dewolf, Charlotte Martin, Dirk Tourwé, Florine Cavelier, Louis Gendron, Philippe Sarret, Mariana Spetea, and Steven Ballet
• [ASAP] Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments
  by Takeshi Yokoyama and Mineyuki Mizuguchi
• [ASAP] Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry
  by Patrick Mäder and Lars Kattner

ACS Medicinal Chemistry Letters

• [ASAP] Chemical Modification of Linkers Provides Stable Linker–Payloads for the Generation of Antibody–Drug Conjugates
  by Yam B. Poudel, Naidu S. Chowdari, Heng Cheng, Christiana I. Iwuagwu, H. Dalton King, Srikanth Kotapati, David Passmore, Richard Rampulla, Arvind Mathur, Gregory Vite, and Sanjeev Gangwar
• [ASAP] Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK
  by Anurag S. Srivastava, Soo Ko, Scott H. Watterson, Mark A. Pattoli, Stacey Skala, Lihong Cheng, Mary T. Obermeier, Rodney Vickery, Lorell N. Discenza, Celia J. D’Arienzo, Kathleen M. Gillooly, Tracy L. Taylor, Claudine Pulicicchio, Kim W. McIntyre, Shiuhang Yip, Peng Li, Dawn Sun, Dauh-Rurng Wu, Jun Dai, Chunlei Wang, Yingru Zhang, Bei Wang, Joseph Pawluczyk, James Kempson, Rulin Zhao, Xiaoping Hou, Richard Rampulla, Arvind Mathur, Michael A. Galella, Luisa Salter-Cid, Joel C. Barrish, Percy H. Carter, Aberra Fura, James R. Burke, and Joseph A. Tino
• [ASAP] Structural Approach to Assessing the Innovativeness of New Drugs Finds Accelerating Rate of Innovation
  by Todd J. Wills and Alan H. Lipkus
• [ASAP] Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the α1β2γ2 GABA_A Receptor
  by Annet E. M. Blom, Justin Y. Su, Lindsay M. Repka, Sarah E. Reisman, and Dennis A. Dougherty
• [ASAP] Antiferroptotic Activity of Phenothiazine Analogues: A Novel Therapeutic Strategy for Oxidative Stress Related Disease
  by Jun Liu, Indrajit Bandyopadhyay, Lei Zheng, Omar M. Khdour, and Sidney M. Hecht
• [ASAP] Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist
  by Xin Li, Hong Wan, Ping Dong, Bin Wang, Lei Zhang, Qiyue Hu, Ting Zhang, Jun Feng, Feng He, Chang Bai, Lianshan Zhang, and Weikang Tao
• [ASAP] <italic toggle="yes">trans</italic>-Fluorine Effect in Cyclopropane: Diastereoselective Synthesis of Fluorocyclopropyl Cabozantinib Analogs
  by Janis Veliks, Melita Videja, Artis Kinens, Raitis Bobrovs, Martins Priede, and Janis Kuka
• [ASAP] <italic toggle="yes">meso</italic>-Thiophenium Porphyrins and Their Zn(II) Complexes: A New Category of Cationic Photosensitizers
  by Zeaul Hoque Mazumdar, Debdulal Sharma, Avinaba Mukherjee, Samita Basu, Pradeep Kumar Shukla, Tarun Jha, and Devashish Sengupta
• [ASAP] Oxetanyl Sulfoxide MMS-350 Ameliorates Pulmonary Fibrosis <italic toggle="yes">In Vitro</italic>, <italic toggle="yes">In Vivo</italic>, and <italic toggle="yes">Ex Vivo</italic>
  by Logan Mlakar, Jessica Lane, Takahisa Takihara, Chaemin Lim, Melissa M. Sprachman, Kayla R. Lloyd, Peter Wipf, and Carol Feghali-Bostwick
• [ASAP] Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium <italic toggle="yes">Vibrio cholerae</italic>
  by Alessandro Bonardi, Alessio Nocentini, Roberta Cadoni, Sonia del Prete, Pascal Dumy, Clemente Capasso, Paola Gratteri, Claudiu T. Supuran, and Jean-Yves Winum

Journal of Natural Products

• [ASAP] Cytotoxic Xanthone Derivatives from the Mangrove-Derived Endophytic Fungus <italic toggle="yes">Peniophora incarnata</italic> Z4
  by Sui Jun Li, Fang Wen Jiao, Wei Li, Xuan Zhang, Wei Yan, and Rui Hua Jiao
• [ASAP] Deuterium Residual Quadrupolar Couplings: Crossing the Current Frontiers in the Relative Configuration Analysis of Natural Products
  by Philippe Lesot, Roberto R. Gil, Philippe Berdagué, and Armando Navarro-Vázquez
• [ASAP] Deciphering the Biosynthesis of TDP-β-<sc>l</sc>-oleandrose in Avermectin
  by Yue Tang, Min Wang, Hua Qin, Xiangxiang An, Zhengyan Guo, Guoliang Zhu, Lixin Zhang, and Yihua Chen
• [ASAP] <italic toggle="yes">S</italic>-Bridged Thioether and Structure-Diversified Angucyclinone Derivatives from the South China Sea-Derived <italic toggle="yes">Micromonospora echinospora</italic> SCSIO 04089
  by Zhuangjie Fang, Xiaodong Jiang, Qingbo Zhang, Liping Zhang, Wenjun Zhang, Chunfang Yang, Haibo Zhang, Yiguang Zhu, and Changsheng Zhang
• [ASAP] Correction to Lamellarin Sulfates from the Pacific Tunicate <italic toggle="yes">Didemnum ternerratum</italic>
  by Joe Bracegirdle, Luke P. Robertson, Paul A. Hume, Michael J. Page, Abigail V. Sharrock, David F. Ackerley, Anthony R. Carroll, and Robert A. Keyzers
• [ASAP] Staprexanthones, Xanthone-Type Stimulators of Pancreatic β-Cell Proliferation from a Mangrove Endophytic Fungus
  by Qi Gan, Chunyu Lin, Changjun Lu, Yimin Chang, Qian Che, Guojian Zhang, Tianjiao Zhu, Qianqun Gu, Zhiqiang Wu, Mingyu Li, and Dehai Li
• [ASAP] Glucose Uptake-Stimulating Galloyl Ester Triterpenoids from <italic toggle="yes">Castanopsis sieboldii</italic>
  by Hyun Woo Kim, Eun Jin Park, Hyo Moon Cho, Jin-Pyo An, Young Won Chin, Jinwoong Kim, Sang Hyun Sung, and Won Keun Oh
• [ASAP] Correction to Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents
  by Pavan K. Bangalore, Siva K. Vagolu, Rakesh K. Bollikanda, Dileep K. Veeragoni, Pallavi C. Choudante, Sunil Misra, Dharmarajan Sriram, Balasubramanian Sridhar, and Srinivas Kantevari
• [ASAP] Cedrol, a Sesquiterpene Alcohol, Enhances the Anticancer Efficacy of Temozolomide in Attenuating Drug Resistance via Regulation of the DNA Damage Response and MGMT Expression
  by Kai-Fu Chang, Xiao-Fan Huang, Jinghua Tsai Chang, Ya-Chih Huang, Wei-Syuan Lo, Chih-Yen Hsiao, and Nu-Man Tsai
• [ASAP] Asaroidoxazines from the Roots of <italic toggle="yes">Asarum asaroides</italic> Induce Apoptosis in Human Neuroblastoma Cells
  by Shinji Ohta, Shiori Oshimo, Emi Ohta, Tatsuo Nehira, Hisashi Ômura, Mylene M. Uy, and Yasuhiro Ishihara