Discovery of ( ±)-3-(1H-pyrazol-1-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazine derivatives with promising in vitro anticoronavirus and antitumoral activity.
Mol Divers
; 26(3): 1357-1371, 2022 Jun.
Article
in English
| MEDLINE | ID: covidwho-1287225
ABSTRACT
A new series of ( ±)-(3-(3,5-dimethyl-1H-pyrazol-1-yl)-6-phenyl-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-7-yl)(phenyl)methanones were efficiently synthesized starting from 4-amino-5-hydrazinyl-4H-1,2,4-triazole-3-thiol 1, acetyl acetone 2, various aromatic and heterocyclic aldehydes 3 and phenacyl bromides 4. All the newly synthesized compounds were tested for their antiviral and antitumoral activity. It was shown that subtle structural variations on the phenyl moiety allowed to tune biological properties toward antiviral or antitumoral activity. Mode-of-action studies revealed that the antitumoral activity was due to inhibition of tubulin polymerization.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Thiadiazines
Language:
English
Journal:
Mol Divers
Journal subject:
Molecular Biology
Year:
2022
Document Type:
Article
Affiliation country:
S11030-021-10258-8
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