大环己六噁唑：氨基烷基取代基对 RNA 和 DNA G-四链体稳定化和细胞毒性的影响。
Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity.
机构信息
Department of Medicinal Chemistry, Rutgers, The State University of New Jersey, Piscataway, NJ 08854-8020, USA.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3150-4. doi: 10.1016/j.bmcl.2010.03.086. Epub 2010 Mar 30.
A series of 24-membered macrocyclic hexaoxazoles containing one or two aminoalkyl substituents was synthesized and evaluated for cytotoxicity and for their ability to selectively stabilize G-quadruplex DNA and RNA. The most cytotoxic analog 4a, with IC(50) values of 25 and 130 nM using KB3-1 and RPMI 8402 cells, is efficacious in vivo in athymic nude mice with a human tumor xenograft from the breast cancer cell line MDA-MB-435.
合成了一系列含有一个或两个氨烷基取代基的 24 元大环己六恶唑，并评估了它们对细胞毒性以及选择性稳定 G-四链体 DNA 和 RNA 的能力。最具细胞毒性的类似物 4a，对 KB3-1 和 RPMI 8402 细胞的 IC50 值分别为 25 和 130 nM，在荷人乳腺癌 MDA-MB-435 细胞系异种移植瘤的裸鼠体内具有疗效。
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