کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365350 981560 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Inhibition of tubulin polymerization by select alkenyldiarylmethanes
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Inhibition of tubulin polymerization by select alkenyldiarylmethanes
چکیده انگلیسی
During studies on the alkenyldiarylmethane (ADAM) class of non-nucleoside reverse transcriptase inhibitors (NNRTIs), analogues were discovered that exhibit low micromolar and submicromolar cytotoxicities. Since the ADAMs are structurally related to the tubulin polymerization inhibitor CC-5079, a set of 14 ADAMs were tested for inhibition of tubulin polymerization in an attempt to identify the biological target responsible for their cytotoxicity. The results indicate that, overall, the ADAMs are poor inhibitors of tubulin polymerization. However, the two most cytotoxic compounds, 15 and 16, are in fact active as inhibitors of tubulin assembly with IC50 values of 3.7 ± 0.3 and 2.8 ± 0.2 μM, respectively, and they both inhibit the binding of colchicine to tubulin. Both compounds were investigated for anticancer activity in the National Cancer Institute's panel of 60 human cancer cell lines, and both compounds consistently displayed submicromolar cytotoxicities with mean-graph midpoint (MGM) values of 0.31 ± 0.08 and 0.47 ± 0.09 μM, respectively.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 2, 15 January 2008, Pages 469-473
نویسندگان
, , , , , , , , ,