Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells
A N Proshin
1
,
T. P. TROFIMOVA
1, 2
,
O N Zefirova
1, 2
,
I V Zhirkina
2
,
D A Skvortsov
2
,
S. O. Bachurin
1
Publication type: Journal Article
Publication date: 2021-03-27
scimago Q3
SJR: 0.305
CiteScore: 2.8
Impact factor: —
ISSN: 10665285, 15739171
General Chemistry
Abstract
New 3,5-disubstituted-1,2,4-thiadiazoles were synthesized and together with a series of their analogs obtained earlier were tested for cytotoxic activity to breast adenocarcinoma MCF-7 and lung carcinoma A 549 cells. The selectivity of cytotoxic action was determined in comparison to etiologically noncancerous breast epithelial cells MCF-10A and lung fibroblasts VA13. From five- to six-fold selectivity of cytotoxic action was revealed for 3,4-dichlorophenyl-{3-[2-(2-morpholin-4-ylethylamino)propyl]-[1,2,4]thiadiazol-5-yl}amine and (2-{5-[(4-diethylami-nobenzyl)pyridin-3-ylmethylamino]-[1,2,4]thiadiazol-3-yl}-1-methylvinyl)-(2,2,6,6-tetra-methylpiperidin-4-yl)amine in the pairs A 549/VA13 and MCF-7/MCF-10A, respectively. Some structure—property relationships for the compounds under study were discussed.
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Proshin A. N. et al. Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells // Russian Chemical Bulletin. 2021. Vol. 70. No. 3. pp. 510-514.
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Proshin A. N., TROFIMOVA T. P., Zefirova O. N., Zhirkina I. V., Skvortsov D. A., Bachurin S. O. Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells // Russian Chemical Bulletin. 2021. Vol. 70. No. 3. pp. 510-514.
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RIS
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TY - JOUR
DO - 10.1007/s11172-021-3116-4
UR - https://doi.org/10.1007/s11172-021-3116-4
TI - Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells
T2 - Russian Chemical Bulletin
AU - Proshin, A N
AU - TROFIMOVA, T. P.
AU - Zefirova, O N
AU - Zhirkina, I V
AU - Skvortsov, D A
AU - Bachurin, S. O.
PY - 2021
DA - 2021/03/27
PB - Springer Nature
SP - 510-514
IS - 3
VL - 70
SN - 1066-5285
SN - 1573-9171
ER -
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@article{2021_Proshin,
author = {A N Proshin and T. P. TROFIMOVA and O N Zefirova and I V Zhirkina and D A Skvortsov and S. O. Bachurin},
title = {Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells},
journal = {Russian Chemical Bulletin},
year = {2021},
volume = {70},
publisher = {Springer Nature},
month = {mar},
url = {https://doi.org/10.1007/s11172-021-3116-4},
number = {3},
pages = {510--514},
doi = {10.1007/s11172-021-3116-4}
}
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MLA
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Proshin, A. N., et al. “Screening of a series of 3,5-disubstituted 1,2,4-thiadiazoles for selectivity of cytotoxic action to cancer cells.” Russian Chemical Bulletin, vol. 70, no. 3, Mar. 2021, pp. 510-514. https://doi.org/10.1007/s11172-021-3116-4.
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