- Synthesis and anti-angiogenic activity of 6-(1,2,4-thiadiazol-5-yl)-3-amino pyridazine derivatives
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General screening for inhibitors of microvessel growth in vitro in the rat aortic ring assay led to the discovery of a novel series of thiadiazole pyridazine compounds with potential anti-angiogenic activity. Chemical optimization produced orally active compounds with potent in vitro and in vivo anti-angiogenesis and anti-tumor activities.
- Bongartz, Jean-Pierre,Stokbroekx, Raymond,Van der Aa, Marcel,Luyckx, Marcel,Willems, Marc,Ceusters, Marc,Meerpoel, Lieven,Smets, Gerda,Jansen, Tine,Wouters, Walter,Bowden, Charlie,Valletta, Lisa,Herb, Mark,Tominovich, Rose,Tuman, Robert
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p. 589 - 591
(2007/10/03)
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- New Synthesis of 1,2,4-Thiadiazoles
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A new synthesis of 1,2,4-thiadiazoles has been developed.N'-(Thioaroyl)- (and N'-arylthiocarbamoyl-) N,N-dimethylamidines, which were prepared in excellent yields by reactions of thioamides (and thioureas) with N,N-dimethylalkanamide dimethyl acetals, rea
- Lin, Yang-i,Lang, S. A.,Petty, Sharon R.
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p. 3750 - 3753
(2007/10/02)
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