期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 10, 期 11, 页码 1537-1542出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00360
关键词
PDE3A; SLFN12; DNMDP; HeLa; SK-MEL-3
资金
- US National Institutes of Health's Molecular Libraries Program Centers Network (MLPCN) [3U45HG005032-05S1]
- Bayer
6-(4-(Diethylamino)-3-nitrophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one, or DNMDP, potently and selectively inhibits phosphodiesterases 3A and 3B (PDE3A and PDE3B) and kills cancer cells by inducing PDE3A/B interactions with SFLN12. The structure-activity relationship (SAR) of DNMDP analogs was evaluated using a phenotypic viability assay, resulting in several compounds with suitable pharmacokinetic properties for in vivo analysis. One of these compounds, BRD9500, was active in an SK-MEL-3 xenograft model of cancer.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据