129618-65-1Relevant academic research and scientific papers
Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing
Lewis, Timothy A.,De Waal, Luc,Wu, Xiaoyun,Youngsaye, Willmen,Wengner, Antje,Kopitz, Charlotte,Lange, Martin,Gradl, Stefan,Ellermann, Manuel,Lienau, Philip,Schreiber, Stuart L.,Greulich, Heidi,Meyerson, Matthew
supporting information, p. 1537 - 1542 (2019/11/11)
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.
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CANCER
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Page/Page column 78, (2014/10/18)
Disclosed are compounds, such as pyridazinones, that can be, inter alia, used for treating cancer.
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors
Edmondson, Scott D.,Mastracchio, Anthony,He, Jiafang,Chung, Christine C.,Forrest, Michael J.,Hofsess, Scott,MacIntyre, Euan,Metzger, Joseph,O'Connor, Naphtali,Patel, Kajal,Tong, Xinchun,Tota, Michael R.,Van Der Ploeg, Lex H. T.,Varnerin, Jeff P.,Fisher, Michael H.,Wyvratt, Matthew J.,Weber, Ann E.,Parmee, Emma R.
, p. 3983 - 3987 (2007/10/03)
Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC50=0.19 nM, 3A IC50=1.3 nM) was selec
