Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1
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https://figshare.com/articles/dataset/Identification_of_Triazolothiadiazoles_as_Potent_Inhibitors_of_the_dCTP_Pyrophosphatase_1/4653970
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资源简介:
The dCTP pyrophosphatase 1 (dCTPase)
is involved in the regulation of the cellular dNTP pool and has been
linked to cancer progression. Here we report on the discovery of a
series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase
inhibitors. Compounds 16 and 18 display
good correlation between enzymatic inhibition and target engagement,
together with efficacy in a cellular synergy model, deeming them as
a promising starting point for hit-to-lead development.
创建时间:
2017-02-15



