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Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors

, : Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors. Bioorganic & Medicinal Chemistry Letters 24(17): 4125-4128

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.


PMID: 25124112

DOI: 10.1016/j.bmcl.2014.07.055

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