Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo [4, 3-b] pyridazin-8-amine derivatives as tankyrase …

…, A Macchiarulo, SA Aaronson, H Schüler…

Index: Liscio, Paride; Carotti, Andrea; Asciutti, Stefania; Karlberg, Tobias; Bellocchi, Daniele; Llacuna, Laura; Macchiarulo, Antonio; Aaronson, Stuart A; Schueler, Herwig; Pellicciari, Roberto; Camaioni, Emidio Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2807 - 2812

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Citation Number: 10

Abstract

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 ...

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