Journal of Medicinal Chemistry, volume 52, issue 14, pages 4380-4390

Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships

Ermoli Antonella 1
Bargiotti Alberto 1
Brasca Maria Gabriella 1
Ciavolella Antonella 1
Colombo Nicoletta 1
Fachin Gabriele 1
Isacchi Antonella 1
Menichincheri Maria 1
MOLINARI Antonio 1
Montagnoli Alessia 1
Pillan Antonio 1
Rainoldi Sonia 1
Sirtori Federico Riccardi 1
SOLA FRANCESCO 1
Thieffine Sandrine 1
Tibolla Marcellino 1
VALSASINA Barbara 1
Volpi Daniele 1
Santocanale Corrado 1
Vanotti Ermes 1
1
 
Nerviano Medical Sciences, Srl viale Pasteur 10, 20014 Nerviano, Milano, Italy
Publication typeJournal Article
Publication date2009-06-25
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor7.3
ISSN00222623, 15204804
Drug Discovery
Molecular Medicine
Abstract
Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure−activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one (1) to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (42), a potent ATP mimetic inhibitor of Cdc7 kinase with IC50 value of 7 nM, is also reported.

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GOST Copy
Ermoli A. et al. Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 14. pp. 4380-4390.
GOST all authors (up to 50) Copy
Ermoli A., Bargiotti A., Brasca M. G., Ciavolella A., Colombo N., Fachin G., Isacchi A., Menichincheri M., MOLINARI A., Montagnoli A., Pillan A., Rainoldi S., Sirtori F. R., SOLA F., Thieffine S., Tibolla M., VALSASINA B., Volpi D., Santocanale C., Vanotti E. Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 14. pp. 4380-4390.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1021/jm900248g
UR - https://doi.org/10.1021%2Fjm900248g
TI - Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships
T2 - Journal of Medicinal Chemistry
AU - Ermoli, Antonella
AU - Bargiotti, Alberto
AU - Brasca, Maria Gabriella
AU - Ciavolella, Antonella
AU - Colombo, Nicoletta
AU - Fachin, Gabriele
AU - Isacchi, Antonella
AU - Menichincheri, Maria
AU - MOLINARI, Antonio
AU - Montagnoli, Alessia
AU - Pillan, Antonio
AU - Rainoldi, Sonia
AU - Sirtori, Federico Riccardi
AU - SOLA, FRANCESCO
AU - Thieffine, Sandrine
AU - Tibolla, Marcellino
AU - VALSASINA, Barbara
AU - Volpi, Daniele
AU - Vanotti, Ermes
AU - Santocanale, Corrado
PY - 2009
DA - 2009/06/25 00:00:00
PB - American Chemical Society (ACS)
SP - 4380-4390
IS - 14
VL - 52
SN - 0022-2623
SN - 1520-4804
ER -
BibTex |
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BibTex Copy
@article{2009_Ermoli,
author = {Antonella Ermoli and Alberto Bargiotti and Maria Gabriella Brasca and Antonella Ciavolella and Nicoletta Colombo and Gabriele Fachin and Antonella Isacchi and Maria Menichincheri and Antonio MOLINARI and Alessia Montagnoli and Antonio Pillan and Sonia Rainoldi and Federico Riccardi Sirtori and FRANCESCO SOLA and Sandrine Thieffine and Marcellino Tibolla and Barbara VALSASINA and Daniele Volpi and Ermes Vanotti and Corrado Santocanale},
title = {Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships},
journal = {Journal of Medicinal Chemistry},
year = {2009},
volume = {52},
publisher = {American Chemical Society (ACS)},
month = {jun},
url = {https://doi.org/10.1021%2Fjm900248g},
number = {14},
pages = {4380--4390},
doi = {10.1021/jm900248g}
}
MLA
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MLA Copy
Ermoli, Antonella, et al. “Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships.” Journal of Medicinal Chemistry, vol. 52, no. 14, Jun. 2009, pp. 4380-4390. https://doi.org/10.1021%2Fjm900248g.
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