Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 11, Pages 1537-1542Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00360
Keywords
PDE3A; SLFN12; DNMDP; HeLa; SK-MEL-3
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Funding
- US National Institutes of Health's Molecular Libraries Program Centers Network (MLPCN) [3U45HG005032-05S1]
- Bayer
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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.
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