- SMYD2 INHIBITORS
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The present disclosure generally relates to compounds having cellular anti-proliferative activities, and more particularly relates to compounds which inhibit the activity of human SMYD2, a SET and MYND domain-containing protein lysine methyltransferase.
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Paragraph 0110
(2016/02/20)
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- From isonitriles to unsaturated NHC complexes of gold, palladium and platinum
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In a modular template synthesis, unsaturated NHC complexes of gold, palladium and platinum were synthesized from simple metal salts, isonitriles and amines with acetal or ketal groups. Upon the addition of amines with tethered acetal or ketal moieties to the metal-activated isonitrile, first nitrogen acyclic carbene (NAC) complexes are formed. These undergo ring closure and elimination to the unsaturated NHC complexes upon addition of acid. This simple strategy opens an attractive and fast approach to NHC complexes of gold, palladium and platinum. The modular approach allows a fast modification and is well-suited for the synthesis of unsymetrically and symmetrically substituted unsaturated NHC complexes.
- Riedel, Dominic,Wurm, Thomas,Graf, Katharina,Rudolph, Matthias,Rominger, Frank,Hashmi, A. Stephen K.
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supporting information
p. 1515 - 1523
(2015/05/19)
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- Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2
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A lack of useful small molecule tools has precluded thorough interrogation of the biological function of SMYD2, a lysine methyltransferase with known tumor-suppressor substrates. Systematic exploration of the structure-activity relationships of a previous
- Sweis, Ramzi F.,Wang, Zhi,Algire, Mikkel,Arrowsmith, Cheryl H.,Brown, Peter J.,Chiang, Gary G.,Guo, Jun,Jakob, Clarissa G.,Kennedy, Steven,Li, Fengling,Maag, David,Shaw, Bailin,Soni, Nirupama B.,Vedadi, Masoud,Pappano, William N.
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supporting information
p. 695 - 700
(2015/06/30)
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- BENZOXAZINONE DERIVATIVES ACTING AS BETA2-ADRENORECEPTOR AGONIST FOR THE TREATMENT OF RESPIRATORY DISORDERS
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The present invention provides a compound of formula (I), wherein W, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 41-42
(2010/01/12)
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- AMINE DERIVATIVES AND THEIR USE IN BETA-2-ADRENORECEPTOR MEDIATED DISEASES
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The present invention provides compounds of formula (I), wherein k, Ar, R2, R3, R4, R5, R4', R5', R6, R7, A, D, m and E are as defined in the specification, processes
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Page/Page column 57
(2008/12/06)
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