کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1355953 | 981077 | 2010 | 10 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and tubulin-binding properties of new allocolchicinoids Synthesis and tubulin-binding properties of new allocolchicinoids](/preview/png/1355953.png)
Allocolchicinoids with B- and C-ring variations were synthesized using sequential enyne-metathesis/ Diels–Alder reactions (A → AB → ABC approach) and evaluated for their inhibitory effect on tubulin assembly in vitro. (−)-Allocolchicine 11 with methyl ester at C10 and (±)-cyclopropyl allocolchicinoid 32 exhibit similar activity than (−)-colchicine (1), probably derived from a similar flexibility in the biphenyl system. The presence of methyl ester at C10 led to a little loss in potency in comparison with the series with methyl ester at C9. A complete loss of activity was observed for allocolchicine 9 with methyl ester at C11.
New allocolchicinoids with B- and C-ring variations were synthesized and evaluated for their inhibitory effect on tubulin assembly.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic Chemistry - Volume 38, Issue 4, August 2010, Pages 149–158