Open Access
Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity
Тип публикации: Journal Article
Дата публикации: 2019-08-25
PubMed ID:
31450696
Organic Chemistry
Drug Discovery
Physical and Theoretical Chemistry
Pharmaceutical Science
Molecular Medicine
Analytical Chemistry
Chemistry (miscellaneous)
Краткое описание
A library of novel 2-(het)arylpyrrolidine-1-carboxamides were obtained via a modular approach based on the intramolecular cyclization/Mannich-type reaction of N-(4,4-diethoxybutyl)ureas. Their anti-cancer activities both in vitro and in vivo were tested. The in vitro activity of some compounds towards M-Hela tumor cell lines was twice that of the reference drug tamoxifen, whereas cytotoxicity towards normal Chang liver cell did not exceed the tamoxifen toxicity. In vivo studies showed that the number of surviving animals on day 60 of observation was up to 83% and increased life span (ILS) was up to 447%. Additionally, some pyrrolidine-1-carboxamides possessing a benzofuroxan moiety obtained were found to effectively suppress bacterial biofilm growth. Thus, these compounds are promising candidates for further development both as anti-cancer and anti-bacterial agents.
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MLA
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ГОСТ
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Smolobochkin A. V. et al. Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity // Molecules. 2019. Vol. 24. No. 17. p. 3086.
ГОСТ со всеми авторами (до 50)
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Smolobochkin A. V., Gazizov A. S., Sazykina M., Akylbekov N., Chugunova E., Sazykin I., Gildebrant A., Voronina J., Burilov A., Karchava S., Klimova M., Voloshina A., Sapunova A., Klimanova E., Sashenkova T., Allayarova U., Balakina A., Mishchenko D. Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity // Molecules. 2019. Vol. 24. No. 17. p. 3086.
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RIS
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TY - JOUR
DO - 10.3390/molecules24173086
UR - https://doi.org/10.3390/molecules24173086
TI - Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity
T2 - Molecules
AU - Smolobochkin, Andrey V.
AU - Gazizov, Almir S.
AU - Sazykina, Marina
AU - Akylbekov, Nurgali
AU - Chugunova, Elena
AU - Sazykin, Ivan
AU - Gildebrant, Anastasiya
AU - Voronina, Julia
AU - Burilov, Alexander
AU - Karchava, Shorena
AU - Klimova, Maria
AU - Voloshina, Alexandra
AU - Sapunova, Anastasia
AU - Klimanova, Elena
AU - Sashenkova, Tatyana
AU - Allayarova, Ugulzhan
AU - Balakina, Anastasiya
AU - Mishchenko, Denis
PY - 2019
DA - 2019/08/25
PB - MDPI
SP - 3086
IS - 17
VL - 24
PMID - 31450696
SN - 1420-3049
ER -
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BibTex (до 50 авторов)
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@article{2019_Smolobochkin,
author = {Andrey V. Smolobochkin and Almir S. Gazizov and Marina Sazykina and Nurgali Akylbekov and Elena Chugunova and Ivan Sazykin and Anastasiya Gildebrant and Julia Voronina and Alexander Burilov and Shorena Karchava and Maria Klimova and Alexandra Voloshina and Anastasia Sapunova and Elena Klimanova and Tatyana Sashenkova and Ugulzhan Allayarova and Anastasiya Balakina and Denis Mishchenko},
title = {Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity},
journal = {Molecules},
year = {2019},
volume = {24},
publisher = {MDPI},
month = {aug},
url = {https://doi.org/10.3390/molecules24173086},
number = {17},
pages = {3086},
doi = {10.3390/molecules24173086}
}
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MLA
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Smolobochkin, Andrey V., et al. “Synthesis of novel 2-(Het)arylpyrrolidine derivatives and evaluation of their anticancer and anti-biofilm activity.” Molecules, vol. 24, no. 17, Aug. 2019, p. 3086. https://doi.org/10.3390/molecules24173086.