Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties
A N Proshin
1
,
T. P. TROFIMOVA
1, 2
,
O N Zefirova
1, 2
,
L. N. Petrova
1
,
D A Skvortsov
2
,
S. O. Bachurin
1
Publication type: Journal Article
Publication date: 2019-12-01
scimago Q3
SJR: 0.305
CiteScore: 2.8
Impact factor: —
ISSN: 10665285, 15739171
General Chemistry
Abstract
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.
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Proshin A. N. et al. Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties // Russian Chemical Bulletin. 2019. Vol. 68. No. 12. pp. 2279-2282.
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Proshin A. N., TROFIMOVA T. P., Zefirova O. N., Petrova L. N., Skvortsov D. A., Bachurin S. O. Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties // Russian Chemical Bulletin. 2019. Vol. 68. No. 12. pp. 2279-2282.
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TY - JOUR
DO - 10.1007/s11172-019-2700-3
UR - https://doi.org/10.1007/s11172-019-2700-3
TI - Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties
T2 - Russian Chemical Bulletin
AU - Proshin, A N
AU - TROFIMOVA, T. P.
AU - Zefirova, O N
AU - Petrova, L. N.
AU - Skvortsov, D A
AU - Bachurin, S. O.
PY - 2019
DA - 2019/12/01
PB - Springer Nature
SP - 2279-2282
IS - 12
VL - 68
SN - 1066-5285
SN - 1573-9171
ER -
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@article{2019_Proshin,
author = {A N Proshin and T. P. TROFIMOVA and O N Zefirova and L. N. Petrova and D A Skvortsov and S. O. Bachurin},
title = {Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties},
journal = {Russian Chemical Bulletin},
year = {2019},
volume = {68},
publisher = {Springer Nature},
month = {dec},
url = {https://doi.org/10.1007/s11172-019-2700-3},
number = {12},
pages = {2279--2282},
doi = {10.1007/s11172-019-2700-3}
}
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MLA
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Proshin, A. N., et al. “Novel 5-N,N-disubstituted-5-amino-3-(2-oxopropyl)-1,2,4-thiadiazoles: synthesis and study of neuroprotective and antiproliferative properties.” Russian Chemical Bulletin, vol. 68, no. 12, Dec. 2019, pp. 2279-2282. https://doi.org/10.1007/s11172-019-2700-3.
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