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新型二芳基醚的合成及其作为抗有丝分裂剂的评价。

Synthesis of novel diaryl ethers and their evaluation as antimitotic agents.

作者信息

In Jin-Kyung, Lee Mi-Sung, Yang Jung-Eun, Kwak Jae-Hwan, Lee Heesoon, Boovanahalli Shanthaveerappa K, Lee Kyeong, Kim Soo Jin, Moon Seung Kee, Lee Sungsook, Choi Nam Song, Ahn Soon Kil, Jung Jae-Kyung

机构信息

College of Pharmacy, Chungbuk National University, Cheongju 361-763, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1799-802. doi: 10.1016/j.bmcl.2006.12.048. Epub 2006 Dec 21.

Abstract

A series of novel diaryl ethers possessing various functional groups were synthesized and evaluated for antiproliferative activity in human myeloid leukemia HL-60 cells. Among the compounds examined, compounds 10, 17, 20, 24, and 33 showed moderate to potent antiproliferative activity. These derivatives were further examined in terms of their abilities to inhibit tubulin polymerization; however, all of the tested compounds were relatively ineffective. The reference compound E7010 with an IC(50) of 0.34 microM exhibited potent antiproliferative activity and significantly inhibited tubulin polymerization in a dose-dependent manner.

摘要

合成了一系列具有不同官能团的新型二芳基醚,并对其在人髓系白血病HL-60细胞中的抗增殖活性进行了评估。在所研究的化合物中,化合物10、17、20、24和33表现出中度至强效的抗增殖活性。进一步研究了这些衍生物抑制微管蛋白聚合的能力;然而,所有测试化合物的效果相对较差。IC(50)为0.34 microM的参考化合物E7010表现出强效的抗增殖活性,并以剂量依赖性方式显著抑制微管蛋白聚合。

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