3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance
Alexander A Titov
1
,
Mauro Niso
2
,
Modesto de Candia
2
,
Maxim S Kobzev
1
,
Alexey V Varlamov
1
,
Tatiana N Borisova
1
,
Leonid G Voskressensky
1
,
Nicola A Colabufo
2
,
Saverio Cellamare
2
,
Leonardo Pisani
2
,
Cosimo D Altomare
2
Publication type: Journal Article
Publication date: 2019-09-20
scimago Q3
wos Q2
SJR: 0.501
CiteScore: 4.8
Impact factor: 3.4
ISSN: 17568919, 17568927
PubMed ID:
31538529
Drug Discovery
Pharmacology
Molecular Medicine
Abstract
Aim: Enamino 3-benzazecine compounds, incorporating the C6-C8 allene system, were synthesized and evaluated in vitro as inhibitors of P-glycoprotein (P-gp) and/or multidrug resistance-associated protein 1 (MRP1), two efflux pumps mainly connected with multidrug resistance (MDR) in cancer cells. Results & methodology: Most of the synthesized compounds were selective P-gp inhibitors in Calcein-AM uptake assay. Structure–activity relationships (SARs) pointed out that CO2Me derivatives are more potent than acetyl derivatives, and 10,11-dimethoxy compounds are five to tenfold more potent inhibitors than the respective unsubstituted compounds, and that the P-gp inhibition potency is mainly related to volume parameters. Conclusion: Nanomolar P-gp inhibitors, such as 23 (IC50 = 4.2 nM), restored the antiproliferative activity of doxorubicin in multidrug-resistant cells. The observed activities showed that 3-benzazecine-based compounds may be promising MDR reversers.
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Total citations:
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Citations from 2024:
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Titov A. A. et al. 3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance // Future Medicinal Chemistry. 2019. Vol. 11. No. 16. pp. 2095-2106.
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Titov A. A., Niso M., Candia M. D., Kobzev M. S., Varlamov A. V., Borisova T. N., Voskressensky L. G., Colabufo N. A., Cellamare S., Pisani L., Altomare C. D. 3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance // Future Medicinal Chemistry. 2019. Vol. 11. No. 16. pp. 2095-2106.
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TY - JOUR
DO - 10.4155/fmc-2019-0037
UR - https://doi.org/10.4155/fmc-2019-0037
TI - 3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance
T2 - Future Medicinal Chemistry
AU - Titov, Alexander A
AU - Niso, Mauro
AU - Candia, Modesto de
AU - Kobzev, Maxim S
AU - Varlamov, Alexey V
AU - Borisova, Tatiana N
AU - Voskressensky, Leonid G
AU - Colabufo, Nicola A
AU - Cellamare, Saverio
AU - Pisani, Leonardo
AU - Altomare, Cosimo D
PY - 2019
DA - 2019/09/20
PB - Taylor & Francis
SP - 2095-2106
IS - 16
VL - 11
PMID - 31538529
SN - 1756-8919
SN - 1756-8927
ER -
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BibTex (up to 50 authors)
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@article{2019_Titov,
author = {Alexander A Titov and Mauro Niso and Modesto de Candia and Maxim S Kobzev and Alexey V Varlamov and Tatiana N Borisova and Leonid G Voskressensky and Nicola A Colabufo and Saverio Cellamare and Leonardo Pisani and Cosimo D Altomare},
title = {3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance},
journal = {Future Medicinal Chemistry},
year = {2019},
volume = {11},
publisher = {Taylor & Francis},
month = {sep},
url = {https://doi.org/10.4155/fmc-2019-0037},
number = {16},
pages = {2095--2106},
doi = {10.4155/fmc-2019-0037}
}
Cite this
MLA
Copy
Titov, Alexander A., et al. “3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance.” Future Medicinal Chemistry, vol. 11, no. 16, Sep. 2019, pp. 2095-2106. https://doi.org/10.4155/fmc-2019-0037.