Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity was written by Buchstaller, Hans-Peter;Anlauf, Uwe;Dorsch, Dieter;Kuhn, Daniel;Lehmann, Martin;Leuthner, Birgitta;Musil, Djordje;Radtki, Daniela;Ritzert, Claudio;Rohdich, Felix;Schneider, Richard;Esdar, Christina. And the article was included in Journal of Medicinal Chemistry in 2019.Category: amides-buliding-blocks This article mentions the following:
Tankyrases 1 and 2 (TNKS1/2) are promising pharmacol. targets which recently gained interest for anticancer therapy in Wnt pathway dependent tumors. 2-Aryl-quinazolinones were identified and optimized into potent tankyrase inhibitors through SAR exploration around the quinazolinone core and the 4′-position of the Ph residue. These efforts were supported by anal. of TNKS X-ray and Watermap structures and resulted in compound 5k(I), a potent, selective tankyrase inhibitor with favorable pharmacokinetic properties. The X-ray structure of I in complex with TNKS1 was solved and confirmed the design hypothesis. Modulation of Wnt pathway activity was demonstrated with this compound in a colorectal xenograft model in vivo. In the experiment, the researchers used many compounds, for example, 6-Chloro-2-aminobenzamide (cas: 54166-95-9Category: amides-buliding-blocks).
6-Chloro-2-aminobenzamide (cas: 54166-95-9) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics