31040-09-2Relevant academic research and scientific papers
Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors
Liscio, Paride,Carotti, Andrea,Asciutti, Stefania,Karlberg, Tobias,Bellocchi, Daniele,Llacuna, Laura,Macchiarulo, Antonio,Aaronson, Stuart A,Schüler, Herwig,Pellicciari, Roberto,Camaioni, Emidio
supporting information, p. 2807 - 2812 (2014/04/17)
Searching for selective tankyrases (TNKSs) inhibitors, a new small series of 6,8-disubstituted triazolo[4,3-b]piridazines has been synthesized and characterized biologically. Structure-based optimization of the starting hit compound NNL (3) prompted us to the discovery of 4-(2-(6-methyl-[1,2,4] triazolo[4,3-b]pyridazin-8-ylamino)ethyl)phenol (12), a low nanomolar selective TNKSs inhibitor working as NAD isostere as ascertained by crystallographic analysis. Preliminary biological data candidate this new class of derivatives as a powerful pharmacological tools in the unraveling of TNKS implications in physiopathological conditions.
Synthese et etude physicochimique des 1,2,4-triazolopyridines et des 1,2,4-triazolopyridines
Bouteau, Brigitte,Lancelot, Jean-Charles,Robba, Max
, p. 1649 - 1651 (2007/10/02)
The synthesis of 1,2,4-triazolo and pyridines 7, 8 was achieved by cyclization of 2-hydrazino-3-nitropyridine 3a with formic acid.The 4,5,6,7-tetrahydro-1,2,4-triazolopyridine 13 and 8-amino-1,2,4-triazolopyridine 9 were obtained by catalytic hydrogenation.The reduction of triazolopyridine 8 using stannous chloride led to the intermediate compound 10 which with acetic anhydride afforded 8-acetylamino-5-chloro-1,2,4-triazolopyridine 10a.The structure of the derivatives was determined by 1H-nmr (DMSO-d6).
