39736-28-2Relevant academic research and scientific papers
NOVEL BICYCLIC HETEROCYCLIC COMPOUND
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Paragraph 0475; 0476, (2018/09/27)
Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like. A compound represented by the formula (I) or a pharmacologically acceptable salt thereof. wherein each symbol is as defined in the DESCRIPTION.
4-Bromo-2-(piperidin-1-yl)thiazol-5-yl-phenyl methanone (12b) inhibits Na+/K+-ATPase and Ras oncogene activity in cancer cells
Lefranc, Florence,Xu, Zhanjie,Burth, Patricia,Mathieu, Véronique,Revelant, Germain,Velho De Castro Faria, Mauro,Noyon, Caroline,Garcia, Diogo Gomes,Dufour, Damien,Bruyère, Céline,Gon?alves-De-Albuquerque, Cassiano Felippe,Van Antwerpen, Pierre,Rogister, Bernard,Hesse, Stéphanie,Kirsch, Gilbert,Kiss, Robert
, p. 213 - 223 (2013/07/25)
The in vitro growth inhibitory activity of 26 thiazoles (including 4-halogeno-2,5-disubtituted-1,3-thiazoles) and 5 thienothiazoles was assessed on a panel of 6 human cancer cell lines, including glioma cell lines. (4-Chloro-2-(piperidin-1-yl)thiazol-5-yl)(phenyl)methanone (12a) and (4-bromo-2-(piperidin-1-yl)thiazol-5-yl)(phenyl)methanone (12b) displayed ~10 times greater in vitro growth inhibitory activity than perillyl alcohol (POH), which therapeutically benefits glioma patients through the inhibition of both alpha-1 Na+/K+-ATPase (NAK) and Ras oncogene activity. The in vitro cytostatic activities (as revealed by quantitative videomicroscopy) displayed by 12a and 12b were independent of the intrinsic resistance to pro-apoptotic stimuli associated with cancer cells. Compounds 12a and 12b displayed relatively similar inhibitory activities on purified guinea pig brain preparations that mainly express NAK alpha-2 and alpha-3 subunits, whereas only compound 12b was efficacious against purified guinea pig kidney preparations that mainly express the NAK alpha-1 subunit, which is also expressed in gliomas, melanomas and non-small-cell lung cancers NSCLCs.
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
Lin, Ronghui,Johnson, Sigmond G.,Connolly, Peter J.,Wetter, Steven K.,Binnun, Eva,Hughes, Terry V.,Murray, William V.,Pandey, Niranjan B.,Moreno-Mazza, Sandra J.,Adams, Mary,Fuentes-Pesquera, Angel R.,Middleton, Steven A.
scheme or table, p. 2333 - 2337 (2009/12/07)
2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular p
Synthesis of substituted [1,3]thiazolo[4,5-b]pyridines and [1,3]thiazolo[4,5-d][1,2,3]triazines
Thomae, David,Perspicace, Enrico,Hesse, Stéphanie,Kirsch, Gilbert,Seck, Pierre
, p. 9309 - 9314 (2008/12/21)
In this work, we described an easy preparation of substituted 4-amino-5-cyano-1,3-thiazoles. These compounds have been used as starting materials to obtain two classes of compounds. New substituted [1,3]thiazolo[4,5-e]pyridines were synthesized in one step via Friedl?nder reaction. Diazotation of 4-amino-5-cyano-1,3-thiazoles afforded 4-chloro[1,3]thiazolo[4,5-d][1,2,3]triazines in one step. The later was substituted by a secondary amine to obtain substituted 4-amino[1,3]thiazolo[4,5-d][1,2,3]triazines.
THIAZOLOPYRIMIDINE KINASE INHIBITORS
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Page/Page column 49-50, (2008/06/13)
The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof, and the use thereof as inhibitors of ATP-protein kinase interactions.
New thiazole compounds having fungicidal activity
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, (2008/06/13)
The invention relates to new thiazole compounds of the general formula STR1 wherein R is an C1 -C12 alkyl group or a phenyl group, which groups are unsubstituted or substituted with halogen, nitro or cyano; R1 is a cyano group; a formyl group; an alkylcarbonyl or alkoxycarbonyl group having 2-5 carbon atoms; or a substituted or non-substituted benzoyl group; R2 is a hydrogen atom; a halogen atom; an amino group; an amino group substituted with 1 or 2 substituents selected from the group consisting of C1 -C4 alkyl, C2 -C5 alkynyl, C2 -C5 alkylcarbonyl and C2 -C5 alkoxycarbonyl; an alkyl, alkoxy, alkylthio, alkylsulphinyl or alkyl-sulphonyl group having 1-4 carbon atoms; or a substituted or non-substituted aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl group; and n is 1 or 2. The new compounds show a fungicidal activity and may be used in particular against plant pathogenic seed fungi and soil fungi.
A New Synthesis of Substituted 4-Amino-1,3-thiazoles
Evers, R.
, p. 604 - 608 (2007/10/02)
In the 5-position substituted 4-amino-2-alkylthio-1,3-thiazoles are prepared in good yields from N-nitro-amidino-dithiocarbamates 1 and α-halogen-carbonylcompounds or chloracetonitrile. 1 reacts with 1,3-dichlor-acetone under formation of adequate bis(1,3
