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新型邻碳硼烷基联苯肟衍生物的合成与生物学评价

Synthesis and biological evaluation of a new series of ortho-carboranyl biphenyloxime derivatives.

作者信息

Jin Guofan, Xiao Fuyan, Liu Ruijiang

机构信息

School of Pharmacy, Jiangsu University, Zhenjiang, 212013, People's Republic of China.

出版信息

Chem Cent J. 2018 Jun 29;12(1):76. doi: 10.1186/s13065-018-0444-z.

DOI:10.1186/s13065-018-0444-z
PMID:29959549
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6026111/
Abstract

(Z,Z')-1,1'-(4-ortho-Caboranyldimethyl)-bis(2-methoxyphenylethan-1-oxime) intermediate 3 was synthesized by a three-step reaction with a final treatment with base to give a new series of ortho-carboranyl biphenyloxime derivatives (4-8). Compounds 7 and 8 showed high solubility and the in vitro study results revealed high levels of accumulation in HeLa cells with higher cytotoxicity and boron uptake compared to L-boronphenylalanine.

摘要

(Z,Z')-1,1'-(4-邻碳硼烷基二甲基)-双(2-甲氧基苯乙酮肟)中间体3通过三步反应合成，最后用碱处理得到一系列新的邻碳硼烷基联苯肟衍生物(4-8)。化合物7和8显示出高溶解度，体外研究结果表明，与L-硼苯丙氨酸相比，它们在HeLa细胞中的积累水平较高，具有更高的细胞毒性和硼摄取量。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/78870ef1da00/13065_2018_444_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/9a927e10efaa/13065_2018_444_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/3d7897eb9198/13065_2018_444_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/7e733c51baa5/13065_2018_444_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/78870ef1da00/13065_2018_444_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/9a927e10efaa/13065_2018_444_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/3d7897eb9198/13065_2018_444_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/7e733c51baa5/13065_2018_444_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0173/6026111/78870ef1da00/13065_2018_444_Fig2_HTML.jpg

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