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Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1

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NIAID Data Ecosystem2026-03-10 收录
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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.

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2017-02-15
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