β-d-Ribofuranose as a Core with a Phosphodiester Moiety as the Enzyme Recognition Site for Codrug Development

IF 4.9 1区化学 Q1 CHEMISTRY, ORGANIC Organic Letters Pub Date : 2024-11-14 DOI:10.1021/acs.orglett.4c03662

Jih Ru Hwu, Avijit Panja, Shwu-Chen Tsay, Wen-Chieh Huang, Shu-Yu Lin, Chen-Sheng Yeh, Wu-Chou Su, Li-Xing Yang, Dar-Bin Shieh

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Abstract

An ideal codrug design should be able to control drug release, offer selectivity during drug delivery, and break down into non-toxic fragments after biodegradation. Our design incorporates d-ribofuranose as the core, with carbamate and carbonate groups as linking joints, a phosphodiester moiety as an enzyme recognition site, and lenalidomide and paclitaxel as the constituent drugs. The codrug synthesis involves seven steps with a 33% overall yield. The target codrug increases its water solubility 685 times versus paclitaxel.

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以β-d-核呋喃糖为核心，以磷酸二酯分子为酶识别位点，开发联用药物

理想的共价药物设计应该能够控制药物释放，在给药过程中提供选择性，并在生物降解后分解成无毒的片段。我们的设计以 d-ribofuranose 为核心，氨基甲酸酯和碳酸酯基团为连接点，磷酸二酯分子为酶识别位点，来那度胺和紫杉醇为组成药物。联用药物的合成包括七个步骤，总产率为 33%。与紫杉醇相比，目标共价药物的水溶性提高了 685 倍。

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.