Steroids, volume 138, pages 91-101
Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series
Zavarzin Igor V
,
Volkova Yulia A
,
Hajra Alakananda
,
Andreeva Olga E.
,
Levina Inna S
,
Zavarzin Igor V.
2
,
Hajra Alakananda
3
,
Andreeva Olga E
1
,
Yadykov Anton V
2
,
Levina I.S.
2
,
Volkova Yulia
2
,
Shirinian Valerii Z.
2
Publication type: Journal Article
Publication date: 2018-10-01
Organic Chemistry
Biochemistry
Molecular Biology
Pharmacology
Clinical Biochemistry
Endocrinology
Abstract
HighlightsSynthesis benzylidenes of the 16‐dehydroprogesterone.Evaluation of antitumor activity against two breast cancer cell lines.Compounds 3e,m,n regulate ER&agr; signaling and reveal p53‐independent mechanism of pro‐apoptotic action in MCF‐7 cells. ABSTRACT Novel benzylidenes (chalcones) of the 16‐dehydroprogesterone series have been characterized and their antitumor activity against two breast cancer cell lines was evaluated. Benzylidenes exhibit significant antiproliferative effect on cells and inhibit cell growth in hormone‐dependent MCF‐7 and hormone‐independent MDA‐MB‐231 breast cancer cell lines. Compound 3d exhibits the highest activity against two breast cancer cell lines, with the IC50 value of about 2 &mgr;M. Compounds 3e,m,n display considerable selectivity for hormone‐dependent breast cancer cells, with the IC50 value lower than 6 &mgr;M. Moreover, these steroidal benzylidenes regulate ER&agr; signaling and reveal p53‐independent mechanism of pro‐apoptotic action in MCF‐7 cells. The new class of antitumor compounds holds promise as the basis for the design of agents for cancer therapy.
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- We do not take into account publications that without a DOI.
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Scherbakov A. M. et al. Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series // Steroids. 2018. Vol. 138. pp. 91-101.
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Scherbakov A. M., Zavarzin I. V., Vorontsova S. K., Hajra A., Andreeva O., Yadykov A. V., Levina I. S., Volkova Y. A., Shirinian V. Z., Zavarzin I. V., Hajra A., Andreeva O. E., Yadykov A. V., Levina I., Volkova Y., Shirinian V. Z. Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series // Steroids. 2018. Vol. 138. pp. 91-101.
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TY - JOUR
DO - 10.1016/j.steroids.2018.06.013
UR - https://doi.org/10.1016%2Fj.steroids.2018.06.013
TI - Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series
T2 - Steroids
AU - Scherbakov, Alexander M.
AU - Zavarzin, Igor V
AU - Vorontsova, Svetlana K
AU - Hajra, Alakananda
AU - Andreeva, Olga E.
AU - Yadykov, Anton V
AU - Levina, Inna S
AU - Volkova, Yulia A
AU - Shirinian, V. Z.
AU - Zavarzin, Igor V.
AU - Hajra, Alakananda
AU - Andreeva, Olga E
AU - Yadykov, Anton V
AU - Levina, I.S.
AU - Volkova, Yulia
AU - Shirinian, Valerii Z.
PY - 2018
DA - 2018/10/01 00:00:00
PB - Elsevier
SP - 91-101
VL - 138
SN - 0039-128X
SN - 1878-5867
ER -
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@article{2018_Scherbakov,
author = {Alexander M. Scherbakov and Igor V Zavarzin and Svetlana K Vorontsova and Alakananda Hajra and Olga E. Andreeva and Anton V Yadykov and Inna S Levina and Yulia A Volkova and V. Z. Shirinian and Igor V. Zavarzin and Alakananda Hajra and Olga E Andreeva and Anton V Yadykov and I.S. Levina and Yulia Volkova and Valerii Z. Shirinian},
title = {Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series},
journal = {Steroids},
year = {2018},
volume = {138},
publisher = {Elsevier},
month = {oct},
url = {https://doi.org/10.1016%2Fj.steroids.2018.06.013},
pages = {91--101},
doi = {10.1016/j.steroids.2018.06.013}
}
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