109113-98-6Relevant articles and documents
Synthesis of imidazothiazole-chalcone derivatives as anticancer and apoptosis inducing agents
Kamal, Ahmed,Dastagiri,Ramaiah, M. Janaki,Reddy, J. Surendranadha,Bharathi, E. Vijaya,Srinivas, Chatla,Pushpavalli,Pal, Dhananjaya,Pal-Bhadra, Manika
experimental part, p. 1937 - 1947 (2011/06/20)
A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with logGI50 values ranging from -7.51 to -4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G 0/G1-phase cell-cycle arrest, down-regulation of G 1-phase cell-cycle regulatory proteins such as cyclin D1 and cyclin E1, and up-regulation of CDK4. Moreover, these compounds elicit the characteristic features of apoptosis such as enhancement in the levels of p53, p21, and p27, suppression of NF-κB, and up-regulation of caspase-9. One of these chalcone derivatives, 3d, is potentially well suited for detailed biological studies, either alone or in combination with existing therapies. Breaking the cycle: We undertook an extensive examination of the ability of a series of new chalcone derivatives to regulate the cell cycle and to induce apoptosis in various cancer cell lines. Compound 3d is a particularly suitable candidate for further detailed biological investigations, especially in the treatment of breast cancer.
TRANS-3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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Page/Page column 43; 81-82, (2009/03/07)
The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
α- or β-Trifluoromethyl epoxysulfones: new C3 reagents for heterocyclisation
Laduron, Frederic,Janousek, Zdenek,Viehe, Heinz, G.
, p. 83 - 86 (2007/10/02)
The syntheses of α- and β-trifluoromethyl epoxysulfones 1 and 2 are described.Compound 1 reacts with nucleophiles and bis-nucleophiles to furnish trifluoromethyl ketones and trifluoromethyl heterocycles in good yield, while its isomer 2 leads to the opposite thiazole regioisomers with thioamides. - Keywords: Trifluoromethyl epoxysulfones; Heterocyclisation; Regioisomers; NMR spectroscopy; IR spectroscopy