| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376624 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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 Ki of 2.2 nM at GnRH-R and an IC50 of 36 μM at CYP3A4.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chen Chen, 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,