856781-64-1Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors
Wilson, Stuart C.,Atrash, Butrus,Barlow, Clare,Eccles, Susan,Fischer, Peter M.,Hayes, Angela,Kelland, Lloyd,Jackson, Wayne,Jarman, Michael,Mirza, Amin,Moreno, Javier,Nutley, Bernard P.,Raynaud, Florence I.,Sheldrake, Peter,Walton, Mike,Westwood, Robert,Whittaker, Steven,Workman, Paul,McDonald, Edward
, p. 6949 - 6965 (2012/01/14)
The cyclin-dependent kinase (CDK) inhibitor seliciclib (1, CYC202) is in phase II clinical development for the treatment of cancer. Here we describe the synthesis of novel purines with greater solubility, lower metabolic clearance, and enhanced potency versus CDKs. These compounds exhibit novel selectivity profiles versus CDK isoforms. Compound αSβR-21 inhibits CDK2/cyclin E with IC50 = 30 nM, CDK7-cyclin H with IC50 = 1.3 μM, and CDK9-cyclinT with IC50 = 0.11 μM; it (CCT68127) inhibits growth of HCT116 colon cancer cells in vitro with GI50 = 0.7 μM; and shows antitumour activity when dosed p.o. at 50 mg/kg to mice bearing HCT116 solid human tumour xenografts.
4,5-Dialkylsubstituted 2-imino-1,3-thiazolidine derivatives as potent inducible nitric oxide synthase inhibitors
Ueda, Shigeo,Terauchi, Hideo,Yano, Akihiro,Matsumoto, Masashi,Kubo, Taeko,Kyoya, Yoko,Suzuki, Kenji,Ido, Motoharu,Kawasaki, Motoji
, p. 4101 - 4116 (2007/10/03)
In the course of our search for selective iNOS inhibitors, we have previously reported that 2-imino-1,3-oxazolidine derivatives (1) and 2-aminothiazole derivatives (2) are selective iNOS inhibitors. In order to find more potent iNOS inhibitors, we focused
Enantiomerically pure [1,2-diamino-1-(4-fluorophenyl)butane]platinum(II) complexes: Synthesis and antitumor activity against MCF-7 and MDA-MB 231 breast cancer and LnCaP/FGC prostate cancer cell lines
Dullin, Anja,Dufrasne, Francois,Gelbcke, Michael,Gust, Ronald
, p. 654 - 667 (2007/10/03)
Enantiomerically pure 1,2-diamino-1-(4-fluorophenyl)butanes were synthesized by stereoselective procedures. The enantiomeric purity was determined by 1H NMR spectroscopy after derivatization with (1R)-myrtenal. For the coordination to platinum,
