Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties
| Autor: | Alexey N. Proshin, Sergey O. Bachurin, Dmitry A. Skvortsov, L. N. Petrova, Olga N. Zefirova, T. P. Trofimova |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
010405 organic chemistry
chemistry.chemical_element General Chemistry Calcium Breast Adenocarcinoma 010402 general chemistry medicine.disease 01 natural sciences 0104 chemical sciences Biochemistry chemistry Thiadiazoles Cell culture Cancer cell Carcinoma medicine skin and connective tissue diseases Cytotoxicity Selectivity |
| Zdroj: | Russian Chemical Bulletin. 68:2279-2282 |
| ISSN: | 1573-9171 1066-5285 |
| DOI: | 10.1007/s11172-019-2700-3 |
| Popis: | A series of eight novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles with diverse lipophilic groups was obtained by reaction of 3-isothiocyanato-5-methylisoxazole with secondary amines. All the compounds of the series (independently on the type of the substituents) were found to be ineffective as inhibitors of calcium ions uptake in synaptosomes of rat cerebral cortex. Screening of the cytotoxicity to four cell lines (breast adenocarcinoma MCF-7, conditionnally normal breast epithelial cells MCF-10A, lung carcinoma A549, non-cancer lung fibroblasts VA13) revealed three compounds with good selectivity to cancer cells MCF-7 in comparison with non-cancer cell line MCF- 10A. These 1,2,4-thiadiazoles can serve as new leads for further study of their antitumor properties. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink