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氟环戊烯基嘧啶的设计、合成及抗癌活性

Design, synthesis, and anticancer activity of fluorocyclopentenyl-pyrimidines.

作者信息

Zhao Long Xuan, Yun Mikyung, Kim Hea Ok, Lee Jeong A, Choi Won Jun, Lee Kang Man, Lee Sang Kook, Lee Young B, Ahn Chang Ho, Jeong Lak Shin

机构信息

Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.

出版信息

Nucleic Acids Symp Ser (Oxf). 2005(49):107-8. doi: 10.1093/nass/49.1.107.

DOI:10.1093/nass/49.1.107
PMID:17150656
Abstract

Novel pyrimidine nucleosides with fluorocyclopentene ring were synthesized from D-ribose via stereoselective Grignard reaction and electrophilic vinyl fluorination as key steps. Among compounds tested, cytosine derivative 15a was found to show high growth inhibition against a broad range of human tumor cell lines.

摘要

以D-核糖为原料，通过立体选择性格氏反应和亲电乙烯基氟化作为关键步骤，合成了含氟环戊烯环的新型嘧啶核苷。在所测试的化合物中，发现胞嘧啶衍生物15a对多种人类肿瘤细胞系具有高度的生长抑制作用。

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