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4-O-鬼臼毒素氨基磺酸盐衍生物作为潜在细胞毒剂的设计与合成

Design and Synthesis of 4-O-Podophyllotoxin Sulfamate Derivatives as Potential Cytotoxic Agents.

作者信息

Bader Ammar, Bkhaitan Majdi M, Abdalla Ashraf N, Abdallah Qasem M A, Ali Hamed I, Sabbah Dima A, Albadawi Ghadeer, Abushaikha Ghassan M

机构信息

Umm Al-Qura University, Makkah 21955, Saudi Arabia.

Biomedical Sciences Unit, Arab American University, Jenin, State of Palestine.

出版信息

Evid Based Complement Alternat Med. 2021 Jan 25;2021:6672807. doi: 10.1155/2021/6672807. eCollection 2021.

DOI:10.1155/2021/6672807
PMID:33574882
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7857870/
Abstract

4-O-Podophyllotoxin sulfamate derivatives were prepared using the natural lignan podophyllotoxin. The prepared compounds were afforded by reacting O-sulfonyl chloride podophyllotoxin with ammonia or aminoaryl/heteroaryl motif. Biological evaluation was performed in human breast cancer (MCF7), ovarian cancer (A2780), colon adenocarcinoma (HT29), and normal lung fibroblast (MRC5) cell lines. Compound exhibited potent inhibitory activity and good selectivity margin. Compounds , and exerted apoptotic effect in MCF7 cells in a dose-dependent manner. The cytotoxicity of the verified compounds was inferior to that of podophyllotoxin.

摘要

使用天然木脂素鬼臼毒素制备了4-O-氨基磺酸鬼臼毒素衍生物。通过使O-磺酰氯鬼臼毒素与氨或氨基芳基/杂芳基基序反应得到所制备的化合物。在人乳腺癌（MCF7）、卵巢癌（A2780）、结肠腺癌（HT29）和正常肺成纤维细胞（MRC5）细胞系中进行了生物学评价。化合物表现出强效抑制活性和良好的选择性。化合物、和在MCF7细胞中以剂量依赖性方式发挥凋亡作用。经证实的化合物的细胞毒性低于鬼臼毒素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/f7a26e26392d/ECAM2021-6672807.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/db5f82fcfa6a/ECAM2021-6672807.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/350987dc0d8e/ECAM2021-6672807.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/55306a61062b/ECAM2021-6672807.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/f7a26e26392d/ECAM2021-6672807.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/db5f82fcfa6a/ECAM2021-6672807.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/350987dc0d8e/ECAM2021-6672807.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/55306a61062b/ECAM2021-6672807.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dbf2/7857870/f7a26e26392d/ECAM2021-6672807.003.jpg

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