A novel arginine methyltransferase inhibitor with cellular activity

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 15, 2007, Pages 4150-4153

  Spannhoff, Astrid ^a   Machmur, Rospita ^b   Heinke, Ralf ^c   Trojer, Patrick ^d   Bauer, Ingo ^e   Brosch, Gerald ^e   Schüle, Roland ^a   Hanefeld, Wolfgang ^b   Sippl, Wolfgang ^c   Jung, Manfred ^a  

^a UNIVERSITY OF FREIBURG   (Germany)

^b PHILIPPS UNIVERSITY MARBURG   (Germany)

^c MARTIN LUTHER UNIVERSITY HALLE WITTENBERG   (Germany)

^d UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY   (United States)

^e INNSBRUCK MEDICAL UNIVERSITY   (Austria)

Author keywords

Arginine methyltransferase; Chromatin; Docking; Histone methyltransferase; PRMT; Virtual screening

Indexed keywords

ARGININE METHYLTRANSFERASE INHIBITOR; ENZYME INHIBITOR; HISTONE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CELL ACTIVITY; HORMONE DEPENDENCE; HUMAN; HUMAN CELL; IC 50;

AMIDES; CELL LINE; ENZYME INHIBITORS; HUMANS; METHYLTRANSFERASES; MODELS, MOLECULAR;

EID: 34347399252     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.05.088     Document Type: Article

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14. Purity and identity of the compounds was assessed by NMR, IR, mass spectrometry and elemental analyses (not shown). The synthesis of (R,S)-N-(3-aminopropyl)-2-sulfanylpropionic acid amide 4 and corresponding analytical data have been described by R. Ortmann, Ph.D. Thesis, University of Marburg, Germany 2001, page 311. The syntheses of (N,N′-ethane-1,2-diyl)di[(R,S)-2-(9-xanthenyl-sulfanyl)propionic acid amide 5, N,N′-(3,6-dioxaoctane-1,8-diyl)-di[(R,S)-2-(9-xanthenylsulfanyl)propionic acid amide 6 and 2-(9-xanthenylsulfanyl)-[N,N-butane-1,4-diyl]propionic acid amide 7 have been described by R. Machmur, Ph.D. Thesis, University of Marburg, Germany 2006, 5 page 182, 6 page 186, 7 page 177, 8 page 242.
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17. Compounds 4-8 are chiral compounds and were tested as racemic mixtures. The docking was carried out with all possible stereoisomers, and comparable docking poses were obtained.
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