Bioorganic and Medicinal Chemistry Letters, volume 43, pages 128055
Antibacterial activity of noscapine analogs
Ivanenkov Yan
1, 2
,
Osterman Ilya A.
,
Kartsev Victor G.
3
,
Bezrukov Dmitry S.
,
Yamidanov Renat S.
2
,
Terentiev Victor A.
2, 4
,
Zainullina L. F.
2
,
Baymiev Andrey Kh.
,
Baymiev Alexey Kh.
2, 5
,
Yu Filyaeva Kseniya
2, 5
,
Matniyazov Rustam T
2
,
Vladimirova Anastasiya A
2
,
Mavzyutov Ayrat R
5
,
Zileeva Zulfia R
2
,
Vakhitova Julia V
2
,
Baymiev Andrey
2, 5
,
Osterman Ilya A
6, 7
,
Bezrukov Dmitry S.
8
1
2
3
InterBioScreen ltd, Chernogolovka 142432, Russia.
|
Publication type: Journal Article
Publication date: 2021-07-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor: 2.7
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The antibacterial properties of close noscapine analogs have not been previously reported. We used our pDualrep2 double-reporter High Throughput Screening (HTS) platform to identify a series of noscapine derivatives with promising antibacterial activity. The platform is based on RPF (SOS-response/DNA damage) and Katushka2S (inhibition of translation) proteins and simultaneously provides information on antibacterial activity and the mechanism of action of small-molecule compounds against E. coli. The most potent compound exhibited an MIC of 13.5µM(6.25µg/ml) and a relatively low cytotoxicity against HEK293 cells (CC50=71µM, selectivity index: ∼5.5). Some compounds from this series induced average Katushka2S reporter signals, indicating inhibition of translation machinery in the bacteria; however, these compounds did not attenuate translation in vitro in a luciferase-based translation assay. The most effective compounds did not significantly arrest the mitotic cycle in HEK293 cells, in contrast to the parent compound in a flow cytometry assay. Several molecules showed activity against clinically relevant gram-negative and gram-positive bacterial strains. Compounds from the discovered series can be reasonably regarded as good templates for further development and evaluation.
Citations by journals
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1
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Mendeleev Communications
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Mendeleev Communications
1 publication, 33.33%
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Psychoactives
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Psychoactives
1 publication, 33.33%
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1
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Citations by publishers
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1
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Elsevier
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Elsevier
1 publication, 33.33%
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Multidisciplinary Digital Publishing Institute (MDPI)
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Multidisciplinary Digital Publishing Institute (MDPI)
1 publication, 33.33%
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1
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Ivanenkov Y. et al. Antibacterial activity of noscapine analogs // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 43. p. 128055.
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Yu Filyaeva K., Dontsova O. A., Bezrukov D. S., Kartsev V. G., Osterman I. A., Terentiev V. A., Marina V. I., Vakhitova J. V., Zainullina L. F., Zileeva Z. R., Mavzyutov A. R., Yamidanov R. S., Vladimirova A. A., Baymiev A. K., Baymiev A. K., Matniyazov R. T., Ivanenkov Y., Baymiev A., Osterman I. A., Bezrukov D. S. Antibacterial activity of noscapine analogs // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 43. p. 128055.
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TY - JOUR
DO - 10.1016/j.bmcl.2021.128055
UR - https://doi.org/10.1016%2Fj.bmcl.2021.128055
TI - Antibacterial activity of noscapine analogs
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Ivanenkov, Yan
AU - Yu Filyaeva, Kseniya
AU - Matniyazov, Rustam T
AU - Baymiev, Andrey Kh.
AU - Baymiev, Alexey Kh.
AU - Vladimirova, Anastasiya A
AU - Yamidanov, Renat S.
AU - Mavzyutov, Ayrat R
AU - Zileeva, Zulfia R
AU - Zainullina, L. F.
AU - Vakhitova, Julia V
AU - Marina, Valeriya I
AU - Terentiev, Victor A.
AU - Osterman, Ilya A.
AU - Kartsev, Victor G.
AU - Bezrukov, Dmitry S.
AU - Dontsova, Olga A.
AU - Baymiev, Andrey
AU - Osterman, Ilya A
AU - Bezrukov, Dmitry S.
PY - 2021
DA - 2021/07/01 00:00:00
PB - Elsevier
SP - 128055
VL - 43
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2021_Ivanenkov,
author = {Yan Ivanenkov and Kseniya Yu Filyaeva and Rustam T Matniyazov and Andrey Kh. Baymiev and Alexey Kh. Baymiev and Anastasiya A Vladimirova and Renat S. Yamidanov and Ayrat R Mavzyutov and Zulfia R Zileeva and L. F. Zainullina and Julia V Vakhitova and Valeriya I Marina and Victor A. Terentiev and Ilya A. Osterman and Victor G. Kartsev and Dmitry S. Bezrukov and Olga A. Dontsova and Andrey Baymiev and Ilya A Osterman and Dmitry S. Bezrukov},
title = {Antibacterial activity of noscapine analogs},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2021},
volume = {43},
publisher = {Elsevier},
month = {jul},
url = {https://doi.org/10.1016%2Fj.bmcl.2021.128055},
pages = {128055},
doi = {10.1016/j.bmcl.2021.128055}
}