Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity
Тип публикации: Journal Article
Дата публикации: 2009-10-21
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
19845386
Drug Discovery
Molecular Medicine
Краткое описание
DHEA analogues with modifications at positions C3 or C17 were synthesized and evaluated for neuroprotective activity against the neural-crest-derived PC12 cell model of serum deprivation-induced apoptosis. The most potent compounds were the spiro-epoxy derivatives 17beta-spiro[5-androstene-17,2'-oxiran]-3beta-ol (20), (20S)-3beta,21-dihydroxy-17beta,20-epoxy-5-pregnene (23), and (20R)-3beta,21-dihydroxy-17alpha,20-epoxy-5-pregnene (27) with IC(50) values of 0.19 +/- 0.01, 99.0 +/- 4.6, and 6.4 +/- 0.3 nM, respectively. Analogues 20, 23, and 27, up to the micromolar range of concentrations, were unable to activate estrogen receptor alpha and beta (ERalpha and ERbeta) or to interfere with ER-dependent gene expression significantly. In addition, they were unable to stimulate the growth of Ishikawa, MCF-7, and LNCaP cells. Our results suggest that the spiro-epoxyneurosteroid derivatives 20, 23, and 27 may prove to be lead molecules for the synthesis of novel neuroprotective agents.
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MLA
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ГОСТ
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Calogeropoulou T. et al. Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 21. pp. 6569-6587.
ГОСТ со всеми авторами (до 50)
Скопировать
Calogeropoulou T., Minas V., Charalampopoulos I., Vergou V., Lazaridis I., Gravanis A. Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 21. pp. 6569-6587.
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RIS
Скопировать
TY - JOUR
DO - 10.1021/jm900468p
UR - https://doi.org/10.1021/jm900468p
TI - Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity
T2 - Journal of Medicinal Chemistry
AU - Calogeropoulou, Theodora
AU - Minas, Vassilios
AU - Charalampopoulos, Ioannis
AU - Vergou, Varvara
AU - Lazaridis, Iakovos
AU - Gravanis, Achille
PY - 2009
DA - 2009/10/21
PB - American Chemical Society (ACS)
SP - 6569-6587
IS - 21
VL - 52
PMID - 19845386
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (до 50 авторов)
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@article{2009_Calogeropoulou,
author = {Theodora Calogeropoulou and Vassilios Minas and Ioannis Charalampopoulos and Varvara Vergou and Iakovos Lazaridis and Achille Gravanis},
title = {Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity},
journal = {Journal of Medicinal Chemistry},
year = {2009},
volume = {52},
publisher = {American Chemical Society (ACS)},
month = {oct},
url = {https://doi.org/10.1021/jm900468p},
number = {21},
pages = {6569--6587},
doi = {10.1021/jm900468p}
}
Цитировать
MLA
Скопировать
Calogeropoulou, Theodora, et al. “Novel Dehydroepiandrosterone Derivatives with Antiapoptotic, Neuroprotective Activity.” Journal of Medicinal Chemistry, vol. 52, no. 21, Oct. 2009, pp. 6569-6587. https://doi.org/10.1021/jm900468p.