کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1357554 | 981258 | 2016 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A derivative of the staurosporine aglycon (K252c), in which the lactam ring was replaced by a pyrazole moiety, was synthesized. The resulting indolopyrazolocarbazole (3) inhibited Pim isoforms 1–3 whereas it did not impair the activity of two known targets of K252c, protein kinase C isoforms α and γ. Compound 3 exhibited moderate cytotoxic activity toward human leukemia and colon carcinoma cell lines (K562 and HCT116), strongly suggesting that this new scaffold deserves further investigations for treatment of malignancies associated with Pim activity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 14, 15 July 2016, Pages 3116–3124
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 14, 15 July 2016, Pages 3116–3124
نویسندگان
Yannick J. Esvan, Francis Giraud, Elisabeth Pereira, Virginie Suchaud, Lionel Nauton, Vincent Théry, Lyubov G. Dezhenkova, Dmitry N. Kaluzhny, Vsevolod N. Mazov, Alexander A. Shtil, Fabrice Anizon, Pascale Moreau,