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新型双蒽醌衍生物的合成及其作为抗肿瘤剂的生物评价。

Synthesis of novel bis-anthraquinone derivatives and their biological evaluation as antitumor agents.

机构信息

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Arch Pharm Res. 2013 May;36(5):573-8. doi: 10.1007/s12272-013-0074-x. Epub 2013 Mar 8.

Abstract

Cancer has become a major worldwide problem and drug resistance now is one of the most important problems in treatment of cancer. Anthraquinone derivatives represent one of the most important drugs that can be used in treatment of many types of cancer. In this study two series of novel bis-anthraquinone derivatives have been synthesized. Five of these compounds were chosen to be evaluated for their antitumor activity against human cancer cell lines by the National Cancer Institute (NCI, USA). Marked activity was shown for the tested compounds(2-6). The most active one was compound 6 with mean value -67.00 against all cell lines. Compounds 7 and 8 were found inactive.

摘要

癌症已成为一个全球性的重大问题,而耐药性是癌症治疗中最重要的问题之一。蒽醌衍生物是可用于治疗多种癌症的最重要药物之一。在这项研究中,合成了两个系列的新型双蒽醌衍生物。选择其中的五种化合物,由美国国立癌症研究所(NCI)评估其对人类癌细胞系的抗肿瘤活性。测试的化合物(2-6)显示出显著的活性。最活跃的化合物是化合物 6,对所有细胞系的平均抑制率为-67.00。化合物 7 和 8 被发现没有活性。

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