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3-(5-phenyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid
inhibitor of protein kinase CK2, IC50 = 0.008M
OTAVAchemicals Catalogue Number: 1156728
CAS Registry Number: 1216956-54-5
Purity: 95%
Ref. 1: Pat. 86041, 2013-12-10. Low-molecular organic ATP-competitive inhibitors of serine/threonine kinase CK2 based on 4-amino-thieno-[2,3-d]pyrimidine heterocycle. Ostrynska O.V., Balanda A., Bdzhola V.G., Kotey I.M. Kharenko P., Yarmoluk S.M.
Ref. 2: Ostrynska OV, Balanda AO, Bdzhola VG, Golub AG, Kotey IM, Kukharenko OP, Gryshchenko AA, Briukhovetska NV, Yarmoluk SM. Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines. Eur. J. Med. Chem., 2016, 115:148-160
Abstract: An extension of our previous research work has resulted in a number of new ATP-competitive CK2 inhibitors that have been identified among 4-aminothieno[2,3-d]pyrimidine derivatives. The most active compounds obtained in the course of the research are 3-(5-p-tolyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5e (NHTP23, IC50 = 0.01 M), 3-(5-phenyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5g (NHTP25, IC50 = 0.065M) and 3-(6-methyl-5-phenyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5n (NHTP33, IC50 = 0.008M). Structureâactivity relationships of the tested 4-aminothieno[2,3-d]pyrimidine derivatives have been studied and their binding mode with ATP-acceptor site of CK2 has been proposed. A negative effect of intramolecular hydrogen bonding in the compoundsâ structure is discussed.
DOI: 10.1016/j.ejmech.2016.03.004
Price info:
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1 MG |
40 EUR |
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5 MG |
90 EUR |
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10 MG |
160 EUR |
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300uL of 10mM solution |
60 EUR
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