170921-49-0Relevant articles and documents
Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening
Stotani, Silvia,Lorenz, Christoph,Winkler, Matthias,Medda, Federico,Picazo, Edwige,Ortega Martinez, Raquel,Karawajczyk, Anna,Sanchez-Quesada, Jorge,Giordanetto, Fabrizio
, p. 330 - 336 (2016/07/06)
The exploration of innovative chemical space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biologically relevant metabolites and show attractive features, such as molecular compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available commercial reagents and robust chemical transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented.
IMIDAZOLIN-5-ONE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER
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, (2015/04/15)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
IMIDAZOLIN-5-ONE DERIVATIVES USEFUL AS FATTY ACID SNTHASE (FASN) INHIBITORS FOR|THE TREATMENT OF CANCER
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, (2014/03/26)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related disorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
Discovery of a highly selective PLD2 inhibitor (ML395): A new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains
O'Reilly, Matthew C.,Oguin, Thomas H.,Scott, Sarah A.,Thomas, Paul G.,Locuson, Charles W.,Morrison, Ryan D.,Daniels, J. Scott,Brown, H. Alex,Lindsley, Craig W.
supporting information, p. 2633 - 2637 (2015/02/02)
Further chemical optimization of the halopemide-derived family of dual phospholipase D1/2 (PLD1/2) inhibitors afforded ML395 (VU0468809), a potent, >80-fold PLD2 selective allosteric inhibitor (cellular PLD1, IC50>30 000 nm; cellular PLD2, IC50=360 nm). Moreover, ML395 possesses an attractive in vitro DMPK profile, improved physiochemical properties, ancillary pharmacology (Eurofins Panel) cleaner than any other reported PLD inhibitor, and has been found to possess interesting activity as an antiviral agent in cellular assays against a range of influenza strains (H1, H3, H5 and H7).
Spiperone: Influence of spiro ring substituents on 5-HT(2A) serotonin receptor binding
Metwally, Kamel A.,Dukat, Malgorzata,Egan, Christina T.,Smith, Carol,DuPre, Ann,Gauthier, Colleen B.,Herrick-Davis, Katharine,Teitler, Milt,Glennon, Richard A.
, p. 5084 - 5093 (2007/10/03)
Spiperone (1) is a widely used pharmacological tool that acts as a potent dopamine D2, serotonin 5-HT(1A), and serotonin 5-HT(2A) antagonist. Although spiperone also binds at 5-HT(2C) receptors, it is one of the very few agents that display som