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一种高效的声化学合成方法，用于制备含1,8-萘啶部分的新型席夫碱、噻唑烷和吡唑烷及其对HePG2细胞系的细胞毒性活性。

An efficient sonochemical synthesis of novel Schiff's bases, thiazolidine, and pyrazolidine incorporating 1,8-naphthyridine moiety and their cytotoxic activity against HePG2 cell lines.

作者信息

Ahmed N S, Alfooty K O, Khalifah S S

机构信息

Chemistry Department, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia ; Medicinal Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt.

Chemistry Department, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia.

出版信息

ScientificWorldJournal. 2014 Feb 25;2014:587059. doi: 10.1155/2014/587059. eCollection 2014.

DOI:10.1155/2014/587059
PMID:24723815
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3956519/
Abstract

Novel Schiff's bases 4a-e, 5a, 5b, and 6, thiazolidine 7a-d, and pyrazolidine 8 have been synthesized using the versatile synthon 4-hydroxy-2,7-dimethyl-1,8-naphthyridine 1. Reactions carried out under ultrasound irradiation showed higher rates and yields than those done under silent conditions. The newly synthesized compounds were evaluated for HepG2 cell growth inhibition. The results obtained revealed that the tested compounds possess inhibitory effect on the growth of HepG2 liver cancer cells. The results were compared to doxorubicin as a reference drug (IC50: 0.04). Compounds 4a and 7b showed the highest inhibition activity against the HepG2 cell line (IC50: 0.047 and 0.041 µM, resp.) among all the tested compounds.

摘要

利用多功能合成子4-羟基-2,7-二甲基-1,8-萘啶1合成了新型席夫碱4a - e、5a、5b和6、噻唑烷7a - d以及吡唑烷8。在超声辐射下进行的反应比在无声条件下进行的反应具有更高的速率和产率。对新合成的化合物进行了HepG2细胞生长抑制评估。所得结果表明，所测试的化合物对HepG2肝癌细胞的生长具有抑制作用。将结果与作为参考药物的阿霉素（IC50：0.04）进行了比较。在所有测试化合物中，化合物4a和7b对HepG2细胞系表现出最高的抑制活性（IC50分别为0.047和0.041 μM）。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/305f72c821b5/TSWJ2014-587059.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/9a3f2f8f47ee/TSWJ2014-587059.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/8b24f6afff66/TSWJ2014-587059.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/daaae33f2e1f/TSWJ2014-587059.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/45422c6c48c4/TSWJ2014-587059.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/305f72c821b5/TSWJ2014-587059.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/9a3f2f8f47ee/TSWJ2014-587059.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/8b24f6afff66/TSWJ2014-587059.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/daaae33f2e1f/TSWJ2014-587059.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/45422c6c48c4/TSWJ2014-587059.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1428/3956519/305f72c821b5/TSWJ2014-587059.sch.003.jpg

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