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乙酰咔唑对单羧酸和双羧酸(相似或不同)及氨基酸的光笼化及其在癌症治疗中的双重药物传递应用。

Photocaging of Single and Dual (Similar or Different) Carboxylic and Amino Acids by Acetyl Carbazole and its Application as Dual Drug Delivery in Cancer Therapy.

机构信息

Department of Chemistry, ‡School of Medical Science and Technology, Indian Institute of Technology Kharagpur , 721302 West Bengal, India.

Biomaterials Group, ⊥Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology , Hyderabad 500007, India.

出版信息

J Org Chem. 2016 Nov 18;81(22):11168-11175. doi: 10.1021/acs.joc.6b02152. Epub 2016 Oct 28.

DOI:10.1021/acs.joc.6b02152
PMID:27754672
Abstract

A new fluorescent photoremovable protecting group (FPRPG) based on acetylcarbazole framework has been explored for the first time release of single and dual (similar or different) substrates from single chromophore. Mechanistic studies of the photorelease process revealed that photorelease of two (similar or different) substrates from acetyl carbazole proceeds via a stepwise pathway. Further, we constructed photoresponsive dual drug delivery system (DDS) to release two different anticancer drugs (caffeic acid and chlorambucil, 1 equiv each). In vitro study reveals that our DDS exhibit excellent properties like biocompatibility, cellular uptake, and photoregulated dual drug release.

摘要

一种基于乙酰咔唑骨架的新型荧光光解保护基团(FPRPG)首次被探索用于从单个发色团中释放单分子和双分子(相似或不同)底物。光解释放过程的机理研究表明,乙酰咔唑上两个(相似或不同)底物的光解释放是通过逐步途径进行的。此外,我们构建了光响应的双药物传递系统(DDS)来释放两种不同的抗癌药物(咖啡酸和苯丁酸氮芥,各 1 当量)。体外研究表明,我们的 DDS 具有良好的性能,如生物相容性、细胞摄取和光调控的双药物释放。

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