ACS Medicinal Chemistry Letters, volume 10, issue 4, pages 601-605
Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition
Assunta Giordano
1, 2
,
Giovanni Forte
2
,
Stefania Terracciano
2
,
A Russo
2
,
Marina Sala
2
,
Maria Carmina Scala
2
,
Catrine Johansson
3
,
Udo C.I. Oppermann
3
,
R. Riccio
2
,
I. Bruno
2
,
Simone Di Micco
2
Publication type: Journal Article
Publication date: 2019-02-25
Journal:
ACS Medicinal Chemistry Letters
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor: 4.2
ISSN: 19485875, 19485875
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
JMJD3 is a member of the KDM6 subfamily and catalyzes the demethylation of lysine 27 on histone H3 (H3K27). This protein was identified as a useful tool in understanding the role of epigenetics in inflammatory conditions and in cancer as well. Guided by a virtual fragment screening approach, we identified the benzoxazole scaffold as a new hit suitable for the development of tighter JMJD3 inhibitors. Compounds were synthesized by a microwave-assisted one-pot reaction under catalyst and solvent-free conditions. Among these, compound 8 presented the highest inhibitory activity (IC50 = 1.22 ± 0.22 μM) in accordance with molecular modeling calculations. Moreover, 8 induced the cycle arrest in S-phase on A375 melanoma cells.
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Citations by publishers
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- We do not take into account publications without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Giordano A. et al. Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition // ACS Medicinal Chemistry Letters. 2019. Vol. 10. No. 4. pp. 601-605.
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Giordano A., Forte G., Terracciano S., Russo A., Sala M., Scala M. C., Johansson C., Oppermann U. C., Riccio R., Bruno I., Di Micco S. Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition // ACS Medicinal Chemistry Letters. 2019. Vol. 10. No. 4. pp. 601-605.
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TY - JOUR
DO - 10.1021/acsmedchemlett.8b00589
UR - https://doi.org/10.1021/acsmedchemlett.8b00589
TI - Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition
T2 - ACS Medicinal Chemistry Letters
AU - Forte, Giovanni
AU - Johansson, Catrine
AU - Sala, Marina
AU - Di Micco, Simone
AU - Giordano, Assunta
AU - Terracciano, Stefania
AU - Russo, A
AU - Scala, Maria Carmina
AU - Oppermann, Udo C.I.
AU - Riccio, R.
AU - Bruno, I.
PY - 2019
DA - 2019/02/25 00:00:00
PB - American Chemical Society (ACS)
SP - 601-605
IS - 4
VL - 10
SN - 1948-5875
SN - 1948-5875
ER -
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@article{2019_Giordano,
author = {Giovanni Forte and Catrine Johansson and Marina Sala and Simone Di Micco and Assunta Giordano and Stefania Terracciano and A Russo and Maria Carmina Scala and Udo C.I. Oppermann and R. Riccio and I. Bruno},
title = {Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition},
journal = {ACS Medicinal Chemistry Letters},
year = {2019},
volume = {10},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/acsmedchemlett.8b00589},
number = {4},
pages = {601--605},
doi = {10.1021/acsmedchemlett.8b00589}
}
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Giordano, Assunta, et al. “Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition.” ACS Medicinal Chemistry Letters, vol. 10, no. 4, Feb. 2019, pp. 601-605. https://doi.org/10.1021/acsmedchemlett.8b00589.