| Literature DB >> 18442910 |
Chen Chen1, Yongsheng Chen, Joseph Pontillo, Zhiqiang Guo, Charles Q Huang, Dongpei Wu, Ajay Madan, Takung Chen, Jenny Wen, Qiu Xie, Fabio C Tucci, Martin Rowbottom, Yun-Fei Zhu, Warren Wade, John Saunders, Haig Bozigian, R Scott Struthers.
Abstract
Incorporation of a carboxylic acid into a series of uracil derivatives as hGnRH-R antagonists resulted in a significant reduction of CYP3A4 inhibitory activity. Highly potent hGnRH antagonists with low CYP3A4 inhibitory liability, such as 8a and 8d, were identified. Thus, 8a had a K(i) of 2.2 nM at GnRH-R and an IC(50) of 36 microM at CYP3A4.Entities:
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Year: 2008 PMID： 18442910 DOI： 10.1016/j.bmcl.2008.04.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823