Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Design, Synthesis, and Bioevaluation of a Novel Hybrid Molecular Pyrrolobenzodiazepine–Anthracenecarboxyimide as a Payload for Antibody–Drug Conjugate
  by Weirong Lai, Shengyan Zhao, Qinhuai Lai, Wei Zhou, Mengdan Wu, Xiaohua Jiang, Xin Wang, Yujia Peng, Xian Wei, Liang Ouyang, Lantu Gou, Hao Chen, Yuxi Wang, and Jinliang Yang
• [ASAP] Think Biologically, Act Chemically
  by Matthew J. LaMarche
• [ASAP] GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor
  by Anna Shiriaeva^, Daejin Park, Gyudong Kim, Yoonji Lee, Xiyan Hou, Dnyandev B. Jarhad, Gibae Kim, Jinha Yu, Young Eum Hyun, Woomi Kim, Zhan-Guo Gao, Kenneth A. Jacobson, Gye Won Han^, Raymond C. Stevens^, Lak Shin Jeong, Sun Choi, and Vadim Cherezov^
• [ASAP] Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[<italic toggle="yes">d</italic>]isoxazoles as Potent and Selective Inhibitors of 11β-Hydroxylase
  by Lina Yin, Youtian Pan, Yuanyuan Xue, Xiaoli Chen, Taiyun You, Jiahui Huang, Qihao Xu, and Qingzhong Hu
• [ASAP] Discovery of Novel cccDNA Reducers toward the Cure of Hepatitis B Virus Infection
  by Dongdong Chen, Xuefei Tan, Wenming Chen, Yongfu Liu, Chao Li, Jun Wu, Jiamin Zheng, Hong C. Shen, Meifang Zhang, Waikwong Wu, Lin Wang, Jing Xiong, Jieyu Dai, Kai Sun, Jitao David Zhang, Kunlun Xiang, Baocun Li, XiaoJu Ni, Qihui Zhu, Lu Gao, Li Wang, and Song Feng
• [ASAP] Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections
  by Natalie Hawryluk, Dale Robinson, Yixing Shen, Graham Kyne, Matthew Bedore, Sanjay Menon, Stacie Canan, Thomas von Geldern, Simon Townson, Suzanne Gokool, Alexandra Ehrens, Marianne Koschel, Nathaly Lhermitte-Vallarino, Coralie Martin, Achim Hoerauf, Geraldine Hernandez, Deepak Dalvie, Sabine Specht, Marc Peter Hübner, and Ivan Scandale
• [ASAP] Beyond Retigabine: Design, Synthesis, and Pharmacological Characterization of a Potent and Chemically Stable Neuronal Kv7 Channel Activator with Anticonvulsant Activity
  by Simona Musella, Lidia Carotenuto, Nunzio Iraci, Giulia Baroli, Tania Ciaglia, Piera Nappi, Manuela Giovanna Basilicata, Emanuela Salviati, Vincenzo Barrese, Vincenzo Vestuto, Giuseppe Pignataro, Giacomo Pepe, Eduardo Sommella, Veronica Di Sarno, Michele Manfra, Pietro Campiglia, Isabel Gomez-Monterrey¥, Alessia Bertamino, Maurizio Taglialatela, Carmine Ostacolo¥, and Francesco Miceli
• [ASAP] Identification of Monosaccharide Derivatives as Potent, Selective, and Orally Bioavailable Inhibitors of Human and Mouse Galectin‑3
  by Chunjian Liu, Prasada Rao Jalagam, Jianxin Feng, Wei Wang, Thiruvenkadam Raja, Mallikarjuna Reddy Sura, Raju K. V. L. P. Manepalli, Bheema Reddy Aliphedi, Santosh Medavarapu, Satheesh K. Nair, Vetrichelvan Muthalagu, Ramesh Natesan, Anuradha Gupta, Brett Beno, Manoranjan Panda, Kaushik Ghosh, Jinal Kaushikkumar Shukla, Harinath Sale, Priyanka Haldar, Narasimharaju Kalidindi, Devang Shah, Dipal Patel, Arvind Mathur, Bruce A. Ellsworth, Dong Cheng, and Alicia Regueiro-Ren
• [ASAP] Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases: Discovery of ACT-672125
  by Eva Caroff, Emmanuel A. Meyer, Päivi Äänismaa, Sylvie Froidevaux, Marcel Keller, and Luca Piali
• [ASAP] Selective Inhibitors of Medium-Size S1′ Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery
  by Sandip Kumar Baidya, Suvankar Banerjee, Nilanjan Adhikari, and Tarun Jha

ACS Medicinal Chemistry Letters

• [ASAP] Structure–Activity Relationship and <italic toggle="yes">In Silico</italic> Evaluation of <italic toggle="yes">cis</italic>- and <italic toggle="yes">trans</italic>-PCPA-Derived Inhibitors of LSD1 and LSD2
  by Hideaki Niwa, Chiduru Watanabe, Shin Sato, Toshiyuki Harada, Hisami Watanabe, Ryo Tabusa||, Shunsuke Fukasawa||, Ayane Shiobara||, Tomoko Hashimoto||, Osamu Ohno||, Kana Nakamura, Keiko Tsuganezawa, Akiko Tanaka, Mikako Shirouzu, Teruki Honma, Kenji Matsuno||, and Takashi Umehara
• [ASAP] Aroylhydrazone Glycoconjugate Prochelators Exploit Glucose Transporter 1 (GLUT1) to Target Iron in Cancer Cells
  by Yu-Shien Sung, Baris Kerimoglu, Aikseng Ooi, and Elisa Tomat
• [ASAP] Fragment Ligands of the m⁶A‑RNA Reader YTHDF2
  by Francesco Nai, Raed Nachawati, František Zálešák, Xiang Wang, Yaozong Li, and Amedeo Caflisch
• [ASAP] 2‑Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRPα Checkpoint
  by Eunsun Park, Kyung-Hee Song, Darong Kim, Minyoung Lee, Nguyen Van Manh, Hee Kim, Ki Bum Hong, Jeewoo Lee, Jie-Young Song, and Soosung Kang
• [ASAP] Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins
  by Linjie Li, Mingbo Su, Weiwei Lu, Hongzhi Song, Jiaxiang Liu, Xin Wen, Yanrui Suo, Jingjing Qi, Xiaomin Luo, Yu-Bo Zhou, Xin-Hua Liao, Jia Li, and Xiaojie Lu
• [ASAP] Turning the Other Cheek: Influence of the <italic toggle="yes">cis</italic>-Tetrafluorocyclohexyl Motif on Physicochemical and Metabolic Properties
  by Yong Wang, Wendy Lee, Yi-Chen Chen, Yuhui Zhou, Emile Plise, Madyson Migliozzi, and James J. Crawford
• [ASAP] Multicomponent Macrocyclic IL-17a Modifier
  by Eman Abdelraheem, Max Lubberink, Wenja Wang, Jingyao Li, Atilio Reyes Romero, Robin van der Straat, Xiaochen Du, Matthew Groves, and Alexander Dömling
• [ASAP] Novel 3‑Aminopyrrolidine and Piperidine Macrocyclic Orexin Receptor Agonists for Treating Sleep Disorders
  by Ram W. Sabnis
• [ASAP] Novel Bcl‑2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2–Beclin 1 Protein–Protein Interaction
  by Xiaonan Dong, Qiren Liang, Yun-Zu Pan, Xiaoyu Wang, Yi-Chun Kuo, Wei-Chung Chiang, Xuewu Zhang, Noelle S. Williams, Josep Rizo, Beth Levine, and Jef K. De Brabander
• [ASAP] Identification of α‑Synuclein Proaggregator: Rapid Synthesis and Streamlining RT-QuIC Assays in Parkinson’s Disease
  by Fumito Takada, Takahito Kasahara, Kentaro Otake, Takamitsu Maru, Masanori Miwa, Kei Muto, Minoru Sasaki, Yoshihiko Hirozane, Masato Yoshikawa, and Junichiro Yamaguchi

Journal of Natural Products

• [ASAP] First Total Synthesis of Reassigned Echinosulfonic Acid D
  by Takumi Abe, Ren Nakajima, Toshiki Yamashiro, and Daisuke Sawada
• [ASAP] Network Pharmacology Research and Dual-omic Analyses Reveal the Molecular Mechanism of Natural Product Nodosin Inhibiting Muscle-Invasive Bladder Cancer <italic toggle="yes">in Vitro</italic> and <italic toggle="yes">in Vivo</italic>
  by Xiaopeng Hao, Huixia Fan, Jian Yang, Jinfu Tang, Junhui Zhou, Yuyang Zhao, Luqi Huang, and Yong Xia
• [ASAP] Cryptic Epoxytiglianes from the Kernels of the Blushwood Tree (<italic toggle="yes">Fontainea picrosperma</italic>)
  by Giuseppina Chianese, Hawraz Ibrahim M. Amin, Chiara Maioli, Paul Reddell, Peter Parsons∧, Jason Cullen∧, Jenny Johns∧, Herlina Handoko∧, Glen Boyle∧, Giovanni Appendino, Orazio Taglialatela-Scafati, and Simone Gaeta
• [ASAP] Antiviral Profiling of C‑18- or C‑19-Functionalized Semisynthetic Abietane Diterpenoids
  by Miguel A. González-Cardenete, Damir Hamulić, Francisco J. Miquel-Leal, Natalia González-Zapata, Orlando J. Jimenez-Jarava, Yaneth M. Brand, Laura C. Restrepo-Mendez, Marlen Martinez-Gutierrez, Liliana A. Betancur-Galvis, and Maria L. Marín
• [ASAP] Syzysamalactone, an Unusual 11-Carbon δ‑Lactone Derivative from the Fresh Ripe Fruits of <italic toggle="yes">Syzygium samarangense</italic> (Wax Apple)
  by Yan-Ping Liu, Zhen Xie, Ruo-Qing Guan, Meng-Ran Du, Ze-Hua Qiao, Xin-Yuan Suo, Ze-Yu Liu, Yuan Bian, Lei Qiang, and Yan-Hui Fu
• [ASAP] Structural Revision of the <italic toggle="yes">Stemona</italic> Alkaloids Tuberostemonine O, Dehydrocroomines A and B, and Dehydrocroomine
  by Jia-Meng Jiang, Ze-Hui Shi, Xue-Wen Yang, Dan Zhu, Bao-Jun Zhao, Yue Gao, Dan Xia, Zhi-Qi Yin, and Ke Pan
• [ASAP] Spicatulides A–G, Phenolic–Monoterpenoid Hybrids from <italic toggle="yes">Chloranthus spicatus</italic>
  by Jun-Su Zhou, Su-Ling Huang, Yuan Gao, Qun-Fang Liu, Ying Leng, Bin Zhou, and Jian-Min Yue
• [ASAP] Reconsideration of the Structures of Stemara-13(14)-en-18-ol and Related Diterpene Natural Products: Vinylic Hydrogen Chemical Shifts Are Key
  by Amy T. Merrill and Dean J. Tantillo
• [ASAP] Moroidin, a Cyclopeptide from the Seeds of <italic toggle="yes">Celosia cristata</italic> That Induces Apoptosis in A549 Human Lung Cancer Cells
  by Xiaoya Xu, Nan Jiang, Shangming Liu, Yang Jin, Yuhan Cheng, Tong Xu, Xin Wang, Yuanhua Liu±, Mingwan Zhang°, Shuhu Du, Junting Fan, and Aixia Zhang
• [ASAP] Nostosin G and Spiroidesin B from the Cyanobacterium <italic toggle="yes">Dolichospermum</italic> sp. NIES-1697
  by Chin-Soon Phan, Jakia Jerin Mehjabin, Andrea Roxanne J. Anas, Masahiro Hayasaka, Reiko Onoki, Juting Wang, Taiki Umezawa, Kenji Washio, Masaaki Morikawa, and Tatsufumi Okino