New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives
Pascal Sonnet
1
,
Patrick Dallemagne
2
,
J. M. Guillon
2
,
Cécile ENGUEHARD
2
,
Silvia Stiebing
2
,
Julien Tanguy
2
,
Ronan Bureau
2
,
Sylvain Rault
2
,
Pierrı̈ck Auvray
3
,
Safa Moslemi
3
,
Pascal Sourdaine
3
,
Gilles-Eric Séralini
3
1
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, UFR des Sciences Pharmaceutiques, Caen, France.
|
2
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, UFR des Sciences Pharmaceutiques, 1, rue Vaubénard, 14032 Caen Cedex, France
|
3
IBBA, Laboratoire de Biochimie et Biologie Moléculaire Esplanade de la Paix, 14032 Caen Cedex, France
|
Publication type: Journal Article
Publication date: 2000-05-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
10882007
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
We report herein the design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives, on the basis of a hypothetical pharmacophore structure designed to fit the catalytic site of the human cytochrome P450 aromatase. The in vitro biological evaluation of these compounds allowed us to point out two new potent non-steroidal aromatase inhibitors, MR 20494 and MR 20492, with IC50 values in the range of 0.1 microM.
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116
Total citations:
116
Citations from 2024:
10
(8.62%)
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GOST
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Sonnet P. et al. New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives // Bioorganic and Medicinal Chemistry. 2000. Vol. 8. No. 5. pp. 945-955.
GOST all authors (up to 50)
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Sonnet P., Dallemagne P., Guillon J. M., ENGUEHARD C., Stiebing S., Tanguy J., Bureau R., Rault S., Auvray P., Moslemi S., Sourdaine P., Séralini G. New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives // Bioorganic and Medicinal Chemistry. 2000. Vol. 8. No. 5. pp. 945-955.
Cite this
RIS
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TY - JOUR
DO - 10.1016/S0968-0896(00)00024-9
UR - https://doi.org/10.1016/S0968-0896(00)00024-9
TI - New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives
T2 - Bioorganic and Medicinal Chemistry
AU - Sonnet, Pascal
AU - Dallemagne, Patrick
AU - Guillon, J. M.
AU - ENGUEHARD, Cécile
AU - Stiebing, Silvia
AU - Tanguy, Julien
AU - Bureau, Ronan
AU - Rault, Sylvain
AU - Auvray, Pierrı̈ck
AU - Moslemi, Safa
AU - Sourdaine, Pascal
AU - Séralini, Gilles-Eric
PY - 2000
DA - 2000/05/01
PB - Elsevier
SP - 945-955
IS - 5
VL - 8
PMID - 10882007
SN - 0968-0896
SN - 1464-3391
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2000_Sonnet,
author = {Pascal Sonnet and Patrick Dallemagne and J. M. Guillon and Cécile ENGUEHARD and Silvia Stiebing and Julien Tanguy and Ronan Bureau and Sylvain Rault and Pierrı̈ck Auvray and Safa Moslemi and Pascal Sourdaine and Gilles-Eric Séralini},
title = {New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives},
journal = {Bioorganic and Medicinal Chemistry},
year = {2000},
volume = {8},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/S0968-0896(00)00024-9},
number = {5},
pages = {945--955},
doi = {10.1016/S0968-0896(00)00024-9}
}
Cite this
MLA
Copy
Sonnet, Pascal, et al. “New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives.” Bioorganic and Medicinal Chemistry, vol. 8, no. 5, May. 2000, pp. 945-955. https://doi.org/10.1016/S0968-0896(00)00024-9.