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近年来抗癌核苷类似物的化学合成与评价进展。

Recent Advances in the Chemical Synthesis and Evaluation of Anticancer Nucleoside Analogues.

机构信息

Lennard-Jones Laboratory, School of Chemical and Physical Sciences, Keele University, Keele, Staffordshire, ST5 5BG, UK.

Medicinal Chemistry Knowledge Center, Stanford ChEM-H, 290 Jane Stanford Way, Stanford, CA 94305, USA.

出版信息

Molecules. 2020 Apr 28;25(9):2050. doi: 10.3390/molecules25092050.

Abstract

Nucleoside analogues have proven to be highly successful chemotherapeutic agents in the treatment of a wide variety of cancers. Several such compounds, including gemcitabine and cytarabine, are the go-to option in first-line treatments. However, these materials do have limitations and the development of next generation compounds remains a topic of significant interest and necessity. Herein, we discuss recent advances in the chemical synthesis and biological evaluation of nucleoside analogues as potential anticancer agents. Focus is paid to 4'-heteroatom substitution of the furanose oxygen, 2'-, 3'-, 4'- and 5'-position ring modifications and the development of new prodrug strategies for these materials.

摘要

核苷类似物已被证明是治疗多种癌症的非常成功的化疗药物。包括吉西他滨和阿糖胞苷在内的几种此类化合物是一线治疗的首选。然而,这些材料确实存在局限性,因此开发下一代化合物仍然是一个非常重要且必要的课题。本文讨论了核苷类似物作为潜在抗癌剂在化学合成和生物评价方面的最新进展。重点介绍了呋喃糖氧 4'-杂原子取代、2'、3'、4'和 5'-位环修饰以及这些材料的新前药策略的发展。

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