249923-17-9Relevant 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
Stereoselective deprotonation of chiral and achiral 2-aminoalkyl carbamates: Synthesis of optically active β-amino alcohols via 1-oxy- substituted alkyllithium intermediates
Schwerdtfeger, J?rg,Kolczewski, Sabine,Weber, Berthold,Fr?hlich, Roland,Hoppe, Dieter
, p. 1573 - 1592 (2007/10/03)
A facile protocol for the electrophilic C-substitution (methylation, acylation, α-hydroxyalkylation, and carboxylation) of several 2-(N,N- dibenzylamino)alkan-1-ols via the carbamates 10 is reported. The stereochemistry of the lithiation is greatly influenced by the complexing diamine. The substrate-directed selection between the diastereotopic a-pro-R and pro-S protons in the TMEDA-assisted deprotonation is largely shifted towards pro-S-selectivity in the presence of (-)-sparteine (4). Each of both diastereomeric series is readily accessible in several cases.
