1. Photoinduced synthesis and antitumor activity of a phakellistatin 18 analog with an isoindolinone fragment.
- Author
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Bao, Yujun, Jiang, Shitian, Zhao, Lishuang, Jin, Yingxue, Yan, Rui, and Wang, Zhiqiang
- Subjects
CYCLIC peptides ,MOLECULAR docking ,NATURAL products ,DRUG development - Abstract
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. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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