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具有改进的抗乳腺癌和结肠癌细胞系活性以及P-糖蛋白、细胞色素p450酶活性预测功能的杂双功能N-聚乙二醇喹啉支架衍生物的创新组合。

Innovational combination of hetero-bifunctional N-PEG quinoline scaffolds derivatives with improved anticancer activity against breast and colon cancer cell lines and P-glycoprotein, cytochrome p450 enzyme activity prediction.

作者信息

Gaidhane Mahesh, Ghatole Ajay, Lanjewar Kushal, Hatzade Kishor

机构信息

Department of Chemistry, Shri Lemdeo Patil Mahavidyalaya, RTMNU, Mandal, MS India.

Department of Chemistry, Dhote Bandhu Science College, RTMNU, Gondia, MS India.

出版信息

Turk J Chem. 2020 Dec 16;44(6):1495-1514. doi: 10.3906/kim-2006-13. eCollection 2020.

DOI:10.3906/kim-2006-13
PMID:33488247
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7763119/
Abstract

Polyethylene glycol (PEG) is a polymer that is widely used as a carrier for drug delivery systems (DDS). A library of N-PEGylated quinoline derivatives of PEG molecular weight 200 was prepared rapidly after the activation of PEGs using maleic anhydride. Quinoline with a polymer backbone is essential as new material. PEG is a water-soluble nonionic polymer approved by food and drug organizations for medicine applications. Because of its nontoxic grapheme, it is widely utilized in numerous biochemical, cosmetic, pharmaceutical, and industrialized applications. The modern SwissADME is a web tool that stretches free admittance to a pool of hasty, yet solid, clarifying models for physicochemical properties, pharmacokinetics, and therapeutic science. The present facile synthetic strategy can be a practical approach for incorporating polymeric carriers conjugated with drug moieties, either in the backbone of the polymer or as a terminal and pendant group on the polymer chains.

摘要

聚乙二醇(PEG)是一种聚合物,被广泛用作药物递送系统(DDS)的载体。在使用马来酸酐活化聚乙二醇后,迅速制备了一系列分子量为200的N-聚乙二醇化喹啉衍生物库。具有聚合物主链的喹啉作为新材料至关重要。聚乙二醇是一种经食品和药物组织批准用于医学应用的水溶性非离子聚合物。由于其无毒的特性,它被广泛应用于众多生物化学、化妆品、制药和工业化应用中。现代的SwissADME是一个网络工具,可免费快速访问一系列用于物理化学性质、药代动力学和治疗科学的可靠的解释模型。目前这种简便的合成策略可能是一种切实可行的方法,用于将与药物部分共轭的聚合物载体纳入聚合物主链,或作为聚合物链上的末端和侧基。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/c6db66644a48/turkjchem-44-1495-fig005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/66ead2d6d4ce/turkjchem-44-1495-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/b2909293ac50/turkjchem-44-1495-fig001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/b51e0fbb8e29/turkjchem-44-1495-fig002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/5cc2bf7af321/turkjchem-44-1495-fig003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/007822b8dd30/turkjchem-44-1495-fig004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/c6db66644a48/turkjchem-44-1495-fig005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/66ead2d6d4ce/turkjchem-44-1495-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/b2909293ac50/turkjchem-44-1495-fig001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/b51e0fbb8e29/turkjchem-44-1495-fig002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/5cc2bf7af321/turkjchem-44-1495-fig003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/007822b8dd30/turkjchem-44-1495-fig004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec77/7763119/c6db66644a48/turkjchem-44-1495-fig005.jpg

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