volume 203 pages 112628

Histone deacetylase inhibitor based prodrugs

Publication typeJournal Article
Publication date2020-10-01
scimago Q1
wos Q1
SJR1.142
CiteScore11.3
Impact factor5.9
ISSN02235234, 17683254
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
Histone deacetylases (HDACs) are a family of enzymes which play important roles in the development and progression of cancers. Inhibition of HDACs has been widely studied as a therapeutic strategy in the discovery of anticancer drugs. HDAC inhibitors (HDACIs) have exhibited potency against a variety of cancer types, and four of them have been approved by the US FDA for cancer treatment. However, the clinical benefits of current HDACIs is limited by the insufficient physicochemical property, selectivity and potency. To improve the clinical potential of HDACIs, the prodrug strategy had been utilized to improve the in vivo pharmacokinetic and pharmacodynamic performances of HDACIs. Enhancements in the stability, water solubility, lipophilicity, oral bioavailability and tumor cell selectivity were reported by various studies. Herein, the development of different kinds of HDACI-based prodrug is summarized for the further structural modification of HDACIs with high potential to be drug candidates.
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GOST |
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GOST Copy
Fan W. et al. Histone deacetylase inhibitor based prodrugs // European Journal of Medicinal Chemistry. 2020. Vol. 203. p. 112628.
GOST all authors (up to 50) Copy
Fan W., Zhang L., Jiang Q., Song W., Yan F., Zhang L. Histone deacetylase inhibitor based prodrugs // European Journal of Medicinal Chemistry. 2020. Vol. 203. p. 112628.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.ejmech.2020.112628
UR - https://doi.org/10.1016/j.ejmech.2020.112628
TI - Histone deacetylase inhibitor based prodrugs
T2 - European Journal of Medicinal Chemistry
AU - Fan, Wenli
AU - Zhang, Lihui
AU - Jiang, Qixao
AU - Song, Weiguo
AU - Yan, Fang
AU - Zhang, Lei
PY - 2020
DA - 2020/10/01
PB - Elsevier
SP - 112628
VL - 203
PMID - 32679451
SN - 0223-5234
SN - 1768-3254
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2020_Fan,
author = {Wenli Fan and Lihui Zhang and Qixao Jiang and Weiguo Song and Fang Yan and Lei Zhang},
title = {Histone deacetylase inhibitor based prodrugs},
journal = {European Journal of Medicinal Chemistry},
year = {2020},
volume = {203},
publisher = {Elsevier},
month = {oct},
url = {https://doi.org/10.1016/j.ejmech.2020.112628},
pages = {112628},
doi = {10.1016/j.ejmech.2020.112628}
}