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
SJR: 0.883
CiteScore: 7.3
Impact factor: 3.5
ISSN: 19485875
PubMed ID:
30996803
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.
Top-30
Journals
|
1
2
3
|
|
|
Frontiers in Chemistry
3 publications, 12.5%
|
|
|
International Journal of Molecular Sciences
2 publications, 8.33%
|
|
|
Journal of Medicinal Chemistry
2 publications, 8.33%
|
|
|
Amino Acids
1 publication, 4.17%
|
|
|
Clinical and Translational Oncology
1 publication, 4.17%
|
|
|
European Journal of Medicinal Chemistry
1 publication, 4.17%
|
|
|
Biochimica et Biophysica Acta - Reviews on Cancer
1 publication, 4.17%
|
|
|
Bioorganic Chemistry
1 publication, 4.17%
|
|
|
Tetrahedron
1 publication, 4.17%
|
|
|
Journal of Chromatography A
1 publication, 4.17%
|
|
|
Molecular Catalysis
1 publication, 4.17%
|
|
|
ChemMedChem
1 publication, 4.17%
|
|
|
Molecular Informatics
1 publication, 4.17%
|
|
|
Journal of Natural Products
1 publication, 4.17%
|
|
|
Zeitschrift fur Naturforschung - Section C Journal of Biosciences
1 publication, 4.17%
|
|
|
Journal of Pharmaceutical Analysis
1 publication, 4.17%
|
|
|
Russian Chemical Reviews
1 publication, 4.17%
|
|
|
Chemistry and Biodiversity
1 publication, 4.17%
|
|
|
Signal Transduction and Targeted Therapy
1 publication, 4.17%
|
|
|
1
2
3
|
Publishers
|
1
2
3
4
5
6
7
8
|
|
|
Elsevier
8 publications, 33.33%
|
|
|
Frontiers Media S.A.
3 publications, 12.5%
|
|
|
Springer Nature
3 publications, 12.5%
|
|
|
Wiley
3 publications, 12.5%
|
|
|
American Chemical Society (ACS)
3 publications, 12.5%
|
|
|
MDPI
2 publications, 8.33%
|
|
|
Walter de Gruyter
1 publication, 4.17%
|
|
|
Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 publication, 4.17%
|
|
|
1
2
3
4
5
6
7
8
|
- 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.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
GOST
Copy
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.
GOST all authors (up to 50)
Copy
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.
Cite this
RIS
Copy
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
PB - American Chemical Society (ACS)
SP - 601-605
IS - 4
VL - 10
PMID - 30996803
SN - 1948-5875
ER -
Cite this
BibTex
Copy
@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}
}
Cite this
MLA
Copy
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.