Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains
  by Michael A. Clegg†‡?, Paul Bamborough†, Chun-wa Chung†, Peter D. Craggs†, Laurie Gordon†, Paola Grandi§, Melanie Leveridge†, Matthew Lindon†?, Gemma M. Liwicki†, Anne-Marie Michon§, Judit Molnar†#, Inmaculada Rioja†, Peter E. Soden†, Natalie H. Theodoulou†‡?, Thilo Werner§, Nicholas C. O. Tomkinson‡, Rab K. Prinjha†, and Philip G. Humphreys*†
• [ASAP] Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase
  by Justin T. Ernst*†, Peggy A. Thompson‡, Christian Nilewski§, Paul A. Sprengeler‡, Samuel Sperry‡, Garrick Packard†, Theodore Michels?, Alan Xiang?, Chinh Tran‡, Christopher J. Wegerski‡, Boreth Eam#, Nathan P. Young¶, Sarah Fish?, Joan Chen‡, Haleigh Howard?, Jocelyn Staunton‡, Jolene Molter‡, Jeff Clarine?, Andres Nevarez?, Gary G. Chiang‡, Jim R. Appleman††, Kevin R. Webster‡‡, and Siegfried H. Reich‡
• [ASAP] Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors
  by Zhuoer Zhi†§, Wenting Zhang†§, Jingchun Yao‡, Yanguo Shang†, Qingjing Hao†, Zhong Liu‡, Yushan Ren‡, Jie Li‡, Guimin Zhang*‡, and Jinxin Wang*†
• [ASAP] Structure–Activity Relationship Study Enables the Discovery of a Novel <bold>Berberine</bold> Analogue as the RXRa Activator to Inhibit Colon Cancer
  by Beibei Xu†, Xunjin Jiang‡, Jing Xiong†, Jun Lan§, Yuan Tian†, Linhai Zhong†, Xinquan Wang§, Ning Xu§, Hanwei Cao†, Wenqing Zhang†, Hao Zhang?, Xiaoting Hong†, Yan-yan Zhan*†, Yandong Zhang*‡, and Tianhui Hu*†
• [ASAP] Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists
  by Maoqun Tian†, Aliaa Abdelrahman†, Younis Baqi‡, Eduardo Fuentes?, Djamil Azazna†, Claudia Spanier†, Sabrina Densborn†, Sonja Hinz†, Ralf Schmid§?, and Christa E. Mu¨ller*†
• [ASAP] Addition of Sialic Acid to Insulin Confers Superior Physical Properties and Bioequivalence
  by Daniel E. K. Kabotso†‡, David Smiley‡, John P. Mayer‡, Vasily M. Gelfanov§, Diego Perez-Tilve?, Richard D. DiMarchi‡, Nicola L. B. Pohl*‡, and Fa Liu*?
• [ASAP] 6-Amino[1,2,5]oxadiazolo[3,4-<italic toggle="yes">b</italic>]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Nonalcoholic Steatohepatitis
  by Joseph M. Salamoun†#, Christopher J. Garcia†#, Stefan R. Hargett‡, Jacob H. Murray†, Sing-Young Chen§, Martina Beretta§, Stephanie J. Alexopoulos§, Divya P. Shah§, Ellen M. Olzomer§, Simon P. Tucker??, Kyle L. Hoehn*‡§, and Webster L. Santos*†
• [ASAP] Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer’s Disease
  by Michal S?a´la†8, Kristen R. Hollinger‡??8, Ajit G. Thomas‡, Ranjeet P. Dash‡?, Carolyn Tallon‡?, Vijayabhaskar Veeravalli‡?, Lyndah Lovell‡, Martin Ko¨gler†, Hubert Hr?ebabecky´†, Elis?ka Procha´zkova´†, Ondr?ej Nes?uta†‡, Amanda Donoghue‡, Jenny Lam‡, Rana Rais*‡?, Camilo Rojas*‡§, Barbara S. Slusher*‡???#??, and Radim Nencka*†
• [ASAP] Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials
  by Papireddy Kancharla*†#, Rozalia A. Dodean‡#, Yuexin Li‡#, Sovitj Pou‡, Brandon Pybus§, Victor Melendez§, Lisa Read§, Charles E. Bane§, Brian Vesely§, Mara Kreishman-Deitrick§, Chad Black§, Qigui Li§, Richard J. Sciotti§, Raul Olmeda§, Thu-Lan Luong§, Heather Gaona§, Brittney Potter§, Jason Sousa§, Sean Marcsisin§, Diana Caridha§, Lisa Xie§, Chau Vuong§, Qiang Zeng§, Jing Zhang§, Ping Zhang§, Hsiuling Lin§, Kirk Butler§, Norma Roncal§, Lacy Gaynor-Ohnstad§, Susan E. Leed§, Christina Nolan§, Frida G. Ceja?, Stephanie A. Rasmussen?, Patrick K. Tumwebaze?, Philip J. Rosenthal?, Jianbing Mu±, Brett R. Bayles?&, Roland A. Cooper?, Kevin A. Reynolds†, Martin J. Smilkstein‡, Michael K. Riscoe†‡, and Jane X. Kelly*†‡
• [ASAP] Emerging siRNA Design Principles and Consequences for Biotransformation and Disposition in Drug Development
  by Sara C. Humphreys*†, Mai B. Thayer†, Jabbar Campbell‡, Wen Li Kelly Chen§, Dan Adams§, Julie M. Lade†, and Brooke M. Rock†

ACS Medicinal Chemistry Letters

• [ASAP] Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer
  by Jun Liang*§, Robert Blake§, Jae Chang§, Lori S. Friedman§, Simon Goodacre£, Steven Hartman§, Ellen Rei Ingalla§, James R. Kiefer§, Tracy Kleinheinz§, Sharada Labadie§, Jun Li§, Kwong Wah LaiG, Jiangpeng LiaoG, Vidhi Mody§, Neville McLean£, Ciara Metcalfe§, Michelle Nannini§, Daniel Otwine§, Yingqing Ran§, Nick Ray£, Fabien Roussel£, Amy Sambrone§, Deepak Sampath§, Maia Vinogradova§, John WaiG, Tao WangG, Kuen Yeap£, Amy Young§, Jason Zbieg§, Birong Zhang§, Xiaoping ZhengG, Yu Zhong§, and Xiaojing Wang§
• [ASAP] Discovery of Novel Nonpeptidic PAR2 Ligands
  by Ilona Klo¨sel, Maximilian F. Schmidt, Jonas Kaindl, Harald Hu¨bner, Dorothee Weikert, and Peter Gmeiner*
• [ASAP] Antitumor Potential of the Isoflavonoids (+)- and (-)-2,3,9-Trimethoxypterocarpan: Mechanism-of-Action Studies
  by Kaio Farias†, Roner F. da Costa‡, Assuero S. Meira†, Jairo Diniz-Filho†, Eveline M. Bezerra‡, Valder N. Freire§, Prue Guest?, Maryam Nikahd?, Xinghua Ma?, Michael G. Gardiner?, Martin G. Banwell*??, Maria da C. F. de Oliveira#, Manoel O. de Moraes†, and Claudia do O´ Pessoa*†
• [ASAP] Evaluation of 3-Dimensionality in Approved and Experimental Drug Space
  by Kathleen E. Prosser, Ryjul W. Stokes, and Seth M. Cohen*
• [ASAP] Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1
  by Alan Rolfe*, Shihua Yao, Toung-Vi Nguyen, Kiyoyuki Omoto, Federico Colombo, Milena Virrankoski, Fre´de´ric H. Vaillancourt, Lihua Yu, Andrew Cook, Dominic Reynolds, Stephanos Ioannidis, Ping Zhu, Nicholas A. Larsen, and David M. Bolduc
• [ASAP] Reply to Comment on “Cysteine-Targeted Insecticides against <italic toggle="yes">A. gambiae</italic> Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors”
  by Rudolf Andrys‡, Lukas Gorecki†§, Jan Korabecny*†§, and Kamil Musilek*‡†?
• [ASAP] Comment on “Cysteine-Targeted Insecticides against <italic toggle="yes">A. gambiae</italic> Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors”
  by Yuan-Ping Pang*
• [ASAP] Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging
  by Xiangmei Jin†, Jun Zhang‡, Xiaoyan Jin†, Lan Liu*‡, and Xizhe Tian*†
• [ASAP] Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel ß-Arrestin Antagonist Activity
  by Elnaz Menhaji-Klotz†, Jessica Ward†, Janice A. Brown‡, Paula M. Loria‡, Carina Tan†, Kevin D. Hesp‡, Keith A. Riccardi‡, John Litchfield†, and Markus Boehm*†
• [ASAP] Polysaccharide-Based Nanoparticles for Two-Step Responsive Release of Antitumor Drug
  by Hong-Guang Fu, Yong Chen, Qilin Yu, and Yu Liu*

Journal of Natural Products

• [ASAP] Limonoids from <italic toggle="yes">Cipadessa baccifera</italic>
  by Jin-Hai Yu†, Hua Zhang†, Bin Zhou†, Flavia M. Zimbres#, Seema Dalal‡, Qun-Fang Liu†, Maria B. Cassera#, and Jian-Min Yue*†
• [ASAP] Precursor-Directed Biosynthesis and Fluorescence Labeling of Clickable Microcystins
  by Julia Moschny†?, Wolfram Lorenzen§, Alexandra Hilfer§, Robert Eckenstaler‡, Stefan Jahns§, Heike Enke§, Dan Enke§, Philipp Schneider?, Ralf A. Benndorf‡, and Timo H. J. Niedermeyer*†?
• [ASAP] Quantum Mechanics-Based Structure Analysis of Cyclic Monoterpene Glycosides from <italic toggle="yes">Rhodiola rosea</italic>
  by Yu Tang†, J. Brent Friesen‡§, David C. Lankin†, James B. McAlpine†, Dejan S. Nikolic´†, Matthias Niemitz?, David S. Seigler?, James G. Graham‡, Shao-Nong Chen†‡, and Guido F. Pauli*†‡
• [ASAP] Eudesmacarbonate, a Eudesmane-Type Sesquiterpene from a Marine Filamentous Cyanobacterial Mat (Oscillatoriales) in the Florida Keys
  by Christina A. Lydon†, Logesh Mathivathanan‡, Juanita Sanchez§, Larissa A. H. dos Santos?, Thomas Sauvage?, Sarath P. Gunasekera?, Valerie J. Paul?, and John P. Berry*†
• [ASAP] Hydroxylated Rotenoids Selectively Inhibit the Proliferation of Prostate Cancer Cells
  by David A. Russell*†§, Hannah R. Bridges‡, Riccardo Serreli‡, Sarah L. Kidd†, Natalia Mateu†, Thomas J. Osberger†, Hannah F. Sore†, Judy Hirst‡, and David R. Spring*†
• [ASAP] Diuretic and Renal Protective Effect of Kaempferol 3-<italic toggle="yes">O</italic>-Alpha-<sc>l</sc>-rhamnoside (Afzelin) in Normotensive and Hypertensive Rats
  by Camile Cecconi Cechinel-Zanchett†, Lui´sa Natha´lia Bolda Mariano†, Thaise Boeing†, Juliana de Carvalho da Costa‡, Lui´sa Mota Da Silva†, Jairo K. Bastos‡, Valdir Cechinel-Filho†, and Priscila de Souza*†
• [ASAP] Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B
  by David L. Kukla†, Juan Canchola†, and Jonathan J. Mills*†
• [ASAP] Biomimetic Synthesis of Oleocanthal, Oleacein, and Their Analogues Starting from Oleuropein, A Major Compound of Olive Leaves
  by Georgia Sarikaki†, Nikoleta Christoforidou†, Nicolas Gaboriaud-Kolar†, Amos B. Smith III?, Ioannis K. Kostakis‡, and Alexios-Leandros Skaltsounis*†
• [ASAP] Exploring the Sequence Diversity of Cyclotides from Vietnamese <italic toggle="yes">Viola</italic> Species
  by Tien T. Dang†§, Lai Y. Chan†§, Yen-Hua Huang†, Linh T. T. Nguyen†, Quentin Kaas†, Tien Huynh‡, and David J. Craik*†
• [ASAP] Biosurfactants from Marine Cyanobacteria Collected in Sabah, Malaysia
  by Jakia Jerin Mehjabin†, Liang Wei†, Julie G. Petitbois†, Taiki Umezawa†‡, Fuyuhiko Matsuda†‡, Charles S. Vairappan§, Masaaki Morikawa†‡, and Tatsufumi Okino*†‡