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3
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4
Design and synthesis of new 7-(N-substituted-methyl)-camptothecin derivatives as potent cytotoxic agents.新型7-(N-取代甲基)-喜树碱衍生物作为强效细胞毒剂的设计与合成
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J Med Chem. 2014 Jul 24;57(14):6008-18. doi: 10.1021/jm5003588. Epub 2014 Jul 8.
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Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.基于铃木耦合反应的7-杂芳基取代喜树碱类似物的合成及其体外细胞毒性评价
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新型含哌嗪基-磺酰脒部分的7-取代喜树碱衍生物的设计、合成及细胞毒性活性

Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.

作者信息

Yang Cheng-Jie, Song Zi-Long, Goto Masuo, Liu Ying-Qian, Hsieh Kan-Yen, Morris-Natschke Susan L, Zhao Yong-Long, Zhang Jun-Xiang, Lee Kuo-Hsiung

机构信息

School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.

Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States.

出版信息

Bioorg Med Chem Lett. 2017 Sep 1;27(17):3959-3962. doi: 10.1016/j.bmcl.2017.07.078. Epub 2017 Jul 29.

DOI:10.1016/j.bmcl.2017.07.078
PMID:28789891
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6421834/
Abstract

In our continuing search for camptothecin (CPT)-derived antitumor drugs, novel 7-substituted CPT derivatives incorporating piperazinyl-sulfonylamidine moieties were designed, synthesized and evaluated for cytotoxicity against five tumor cell lines (A-549, MDA-MB-231, MCF-7, KB, and KB-VIN). All of the derivatives showed promising in vitro cytotoxic activity against the tested tumor cell lines, and were more potent than irinotecan. Remarkably, most of the compounds exhibited comparable cytotoxicity against the multidrug-resistant (MDR) KB-VIN and parental KB tumor cell lines, while irinotecan lost activity completely against KB-VIN. Especially, compounds 13r and 13p (IC 0.38 and 0.85μM, respectively) displayed the greatest cytotoxicity against the MDR KB-VIN cell line and merit further development into preclinical and clinical drug candidates for treating cancer, including MDR phenotype.

摘要

在我们持续寻找喜树碱（CPT）衍生的抗肿瘤药物的过程中，设计、合成了新型的含有哌嗪基磺酰脒部分的7-取代CPT衍生物，并评估了它们对五种肿瘤细胞系（A-549、MDA-MB-231、MCF-7、KB和KB-VIN）的细胞毒性。所有衍生物对测试的肿瘤细胞系均显示出有前景的体外细胞毒性活性，且比伊立替康更有效。值得注意的是，大多数化合物对多药耐药（MDR）的KB-VIN和亲本KB肿瘤细胞系表现出相当的细胞毒性，而伊立替康对KB-VIN完全失去活性。特别是，化合物13r和13p（IC分别为0.38和0.85μM）对MDR KB-VIN细胞系表现出最大的细胞毒性，值得进一步开发成为治疗癌症（包括MDR表型）的临床前和临床候选药物。