Photoinduced synthesis and antitumor activity of a phakellistatin 18 analog with an isoindolinone fragment

Autor:	Shitian Jiang, Lishuang Zhao, Yingxue Jin, Rui Yan, Zhiqiang Wang, Yujun Bao
Rok vydání:	2020
Předmět:	Antitumor activity chemistry.chemical_classification 010405 organic chemistry Stereochemistry General Chemistry AutoDock 010402 general chemistry 01 natural sciences Catalysis Cyclic peptide 0104 chemical sciences Mdm2 Protein Drug development chemistry Materials Chemistry Phakellistatin 2
Zdroj:	New Journal of Chemistry. 44:19174-19178
ISSN:	1369-9261 1144-0546
DOI:	10.1039/d0nj03005h
Popis:	Cyclic peptides have become a powerful modality in drug development. Naturally isolated cyclic peptides such as phakellistatins have been found to have broad-spectrum bioactivity. In this paper, we have prepared an analog of phakellistatin 18, and tried to compare its bioactivity with that of our reported phakellistatin 2 analog. It was found that compound 1 derived from phakellistatin 18 showed inferior inhibiting ability compared to the phakellistatin 2 analog, similar to the phenomenon observed in the natural products (phakellistatin 2 presented stronger antitumor activity than that of phakellistatin18). We have performed molecular docking of the two analogs with the MDM2 protein using AutoDock Tools, which showed that the phakellistatin 2 analog presented stronger binding through a H-bond, providing an explanation for the bioactivity difference.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::643cd21e27a3b74d5833193a147ee00b https://doi.org/10.1039/d0nj03005h Zobrazit plný text záznamu