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• W2049767029 abstract "A series of novel thiadiazole amide derivatives have been synthesized and evaluated for inhibitory activities against Cdc25B and PTP1B. Most of them showed inhibitory activities against Cdc25B (IC50 = 1.18–8.01 μg/mL) and PTP1B (IC50 = 0.85–8.75 μg/mL), respectively. Moreover, compounds 5b and 4l were most potent with IC50 values of 1.18 and 0.85 μg/mL for Cdc25B and PTP1B, respectively, compared with reference drugs Na3VO4 (IC50 = 0.93 μg/mL) and oleanolic acid (IC50 = 0.85 μg/mL). The results of selectivity experiments showed that the target compounds were selective inhibitors against PTP1B and Cdc25B. Enzyme kinetic experiments demonstrated that compound 5k was a specific inhibitor with the typical characteristics of a mixed inhibitor." @default.
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• W2049767029 date "2014-09-01" @default.
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• W2049767029 title "Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors" @default.
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• W2049767029 doi "https://doi.org/10.1016/j.bmcl.2014.07.055" @default.
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