Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators

…, JP Northrop, B Bin, JK Dickson, T Stouch…

文献索引：Guengoer, Timur; Chen, Ying; Golla, Rajasree; Ma, Zhengping; Corte, James R.; Northrop, John P.; Bin, Bin; Dickson, John K.; Stouch, Terry; Zhou, Rong; Johnson, Susan E.; Seethala, Ramakrishna; Feyen, Jean H. M. Journal of Medicinal Chemistry, 2006 , vol. 49, # 8 p. 2440 - 2455

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被引用次数: 55

摘要

On the basis of the stucture of genistein, a new series of 3-arylquinazolines was prepared and tested for their estrogen receptor (ER) α and β affinities. 5, 7-Dihydroxy-3-(4- hydroxyphenyl)-4 (3 H)-quinazolinone (1aa) acts as an agonist on both ER subtypes. It has 62-fold higher binding affinity [IC50 (ERβ)= 179 nM] and 38-fold higher functional potency in a transcription assay [EC50 (ERβ)= 76 nM] with ERβ than with ERα, thus improving upon ...