کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10590951 | 981734 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of thiadiazole amide derivatives have been synthesized and evaluated for inhibitory activity 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, respectively, which activities are comparable 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 17, 1 September 2014, Pages 4125-4128
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 17, 1 September 2014, Pages 4125-4128
نویسندگان
Yingjun Li, Yang Yu, Kun Jin, Lixin Gao, Tongchuan Luo, Li Sheng, Xin Shao, Jia Li,