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基于海洋天然产物的抗癌嵌合体分子的设计与合成。

Design and Synthesis of Anti-Cancer Chimera Molecules Based on Marine Natural Products.

机构信息

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju Daero 501, Jinju 52828, Gyeongnam, Korea.

出版信息

Mar Drugs. 2019 Aug 27;17(9):500. doi: 10.3390/md17090500.

DOI:10.3390/md17090500
PMID:31461968
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6780274/
Abstract

In this paper, the chemical conjugation of marine natural products with other bioactive molecules for developing an advanced anti-cancer agent is described. Structural complexity and the extraordinary biological features of marine natural products have led to tremendous research in isolation, structural elucidation, synthesis, and pharmacological evaluation. In addition, this basic scientific achievement has made it possible to hybridize two or more biologically important skeletons into a single compound. The hybridization strategy has been used to identify further opportunities to overcome certain limitations, such as structural complexity, scarcity problems, poor solubility, severe toxicity, and weak potency of marine natural products for advanced development in drug discovery. Further, well-designed marine chimera molecules can function as a platform for target discovery or degradation. In this review, the design, synthesis, and biological evaluation of recent marine chimera molecules are presented.

摘要

本文描述了将海洋天然产物与其他生物活性分子进行化学偶联，以开发先进的抗癌药物。海洋天然产物的结构复杂性和非凡的生物学特性促使人们进行了大量的分离、结构阐明、合成和药理学评价方面的研究。此外，这一基础科学成果使得将两种或更多具有重要生物学意义的骨架杂交到单个化合物中成为可能。杂交策略已被用于进一步发现克服某些局限性的机会，例如海洋天然产物的结构复杂性、稀缺性问题、较差的溶解度、严重的毒性和弱效力，以促进药物发现的进一步发展。此外，设计良好的海洋嵌合体分子可以作为发现或降解目标的平台。在本文中，介绍了最近海洋嵌合体分子的设计、合成和生物学评价。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3de3/6780274/8513ad853e8e/marinedrugs-17-00500-sch013.jpg
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