том 10 издание 4 страницы 601-605

Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition

Тип публикацииJournal Article
Дата публикации2019-02-25
scimago Q1
wos Q2
БС1
SJR0.805
CiteScore5.8
Impact factor4.0
ISSN19485875
Organic Chemistry
Drug Discovery
Biochemistry
Краткое описание
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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ГОСТ |
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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.
ГОСТ со всеми авторами (до 50) Скопировать
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.
RIS |
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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 - Giordano, Assunta
AU - Forte, Giovanni
AU - Terracciano, Stefania
AU - Russo, A
AU - Sala, Marina
AU - Scala, Maria Carmina
AU - Johansson, Catrine
AU - Oppermann, Udo C.I.
AU - Riccio, R.
AU - Bruno, I.
AU - Di Micco, Simone
PY - 2019
DA - 2019/02/25
PB - American Chemical Society (ACS)
SP - 601-605
IS - 4
VL - 10
PMID - 30996803
SN - 1948-5875
ER -
BibTex |
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BibTex (до 50 авторов) Скопировать
@article{2019_Giordano,
author = {Assunta Giordano and Giovanni Forte and Stefania Terracciano and A Russo and Marina Sala and Maria Carmina Scala and Catrine Johansson and Udo C.I. Oppermann and R. Riccio and I. Bruno and Simone Di Micco},
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}
}
MLA
Цитировать
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.