Synthesis and Primary Biological Evaluation of Triazole-Modified Picroside II Compounds
ChemistrySelect
; 6(48):14027-14038, 2021.
Article
in English
| Scopus | ID: covidwho-1599370
ABSTRACT
Picroside II, an iridoid glycoside, has anti-cancer, anti-virus, anti-apoptotic, nervous and myocardial protection effects and so on. However, the oral bioavailability of Picroside II is low, and the half-life in vivo is short, so it is limited to use in clinic. Triazole is a highly stable heterocyclic ring, which can be interacted with various enzymes or receptors in the organism through non-covalent interactions, and many of its good pharmacological activities in vitro and in vivo have been reported. Based on the advantages of triazole and Picroside II, a series of triazole-modified Picroside II derivatives (5 a–5 i) were synthesized by using drug combination principles for the first time. The structures were confirmed by different spectroscopic techniques including 1H NMR, 13C NMR and HRMS, and the primary biological evaluation of anti-breast cancer, anti-colorectal cancer, the effect on SARS-CoV-2 3CLpro inhibitor, and CD47-SIRPα protein were screened as well. Compound 5 e has anti-breast cancer activity, and compounds 3 and 5 i have anti-colorectal cancer activity. © 2021 Wiley-VCH GmbH
Full text:
Available
Collection:
Databases of international organizations
Database:
Scopus
Type of study:
Experimental Studies
Language:
English
Journal:
ChemistrySelect
Year:
2021
Document Type:
Article
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