249922-61-0Relevant articles and documents
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 (2004)
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
Synthesis and in vitro antimycobacterial activity of compounds derived from (R)- and (S)-2-amino-1-butanol - The crucial role of the configuration
Dobrikov, Georgi M.,Valcheva, Violeta,Stoilova-Disheva, Margarita,Momekov, Georgi,Tzvetkova, Pavleta,Chimov, Angel,Dimitrov, Vladimir
supporting information; experimental part, p. 45 - 56 (2012/03/26)
The synthesis of 47 structurally diverse compounds incorporating the (R)-2-amino-1-butanol motif has been realized. Ten of these compounds were found to exhibit in vitro specific activity against Mycobacterium tuberculosis H37Rv in a MIC range of 0.65 μM-14.03 μM. Five of the most active compounds 11, 22, 23, 31 and 42 (5.7-11.1 fold more active than ethambutol) can be outlined with very low cytotoxicity towards human embryonal kidney non-tumour cells (SI ranging from 91.2 to 375.4). For the purpose of comparison the (S)-enantiomers of these most active compounds have been synthesized and evaluated towards M. tuberculosis H37Rv showing no activity even at 20-32 fold higher concentrations.
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
experimental part, 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.
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,
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.
