Novel Isoindolinone-Based Analogs of the Natural Cyclic Peptide Fenestin A: Synthesis and Antitumor Activity
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Le résumé fourni par la source
Small- and medium-sized cyclopeptides have been found to have extensive bioactivities and have drawn much attention from medicinal chemists. In the work described in this paper, various cyclic peptide analogs of Fenestin A were synthesized by intramolecular photoinduced electron-transfer cyclization reactions to study the influence of slight structural changes on the bioactivity of small cyclopeptides. The incorporation of thiazole and rigid isoindolinone fragments was found to improve the bioactivity of the cyclopeptide. Detailed in vitro studies of the apoptosis mechanism, mitochondrial membrane potential, cell cycle, intracellular Ca 2+ concentration, and lactate dehydrogenase activity following treatment with a cyclopeptide showed that the cyclopeptide could induce apoptosis of tumor cells and lead to cycle arrest in the G2/M phase. The research also suggested that the photoinduced reaction could be applied to construct cyclic peptides stereoselectively, and the introduction of rigid fragments could enhance the biological activity of cyclopeptide drugs.
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Le contrôle bibliographique ouvert
DOI retrouvé dans Crossref DOI retrouvé ; titre concordant.
- Titre Crossref
- Novel Isoindolinone-Based Analogs of the Natural Cyclic Peptide Fenestin A: Synthesis and Antitumor Activity
- Date Crossref
- 29/06/2022
- Éditeur
- American Chemical Society (ACS)
- Type
- journal-article
Ce recoupement confirme des métadonnées liées au DOI. Il ne confirme ni la méthode ni les conclusions de l’étude, et il ne compte pas comme une seconde source scientifique indépendante.
Où se fait cette recherche
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Harbin Normal University pays non établi dans la noticeUniversité ou école supérieure
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Qiqihar Medical University Institute of Medicine and Drug Research pays non établi dans la noticeUniversité ou école supérieure
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College of Chemistry & Chemical Engineering Key Laboratory for Photonic and Electronic Bandgap Materials (Ministry of Education) pays non établi dans la noticeUniversité ou école supérieure
Harbin Normal University, Institute of Medicine and Drug Research — Qiqihar Medical University et Key Laboratory for Photonic and Electronic Bandgap Materials (Ministry of Education) — College of Chemistry & Chemical Engineering.
Une affiliation ne permet pas de déduire la nationalité d’un auteur.