2. Academic Validation
  3. Histone deacetylase inhibitor based prodrugs

Histone deacetylase inhibitor based prodrugs

  • Eur J Med Chem. 2020 Oct 1:203:112628. doi: 10.1016/j.ejmech.2020.112628.
Wenli Fan 1,  Lihui Zhang 2,  Qixao Jiang 3,  Weiguo Song 1,  Fang Yan 4,  Lei Zhang 5
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Weifang Medical University, Weifang, Shandong, China.
  • 2 School of Stomatology, Weifang Medical University, Weifang, Shandong, China.
  • 3 Department of Toxicology, School of Public Health, Qingdao University, Qingdao, Shandong, China.
  • 4 Department of Medicinal Chemistry, School of Pharmacy, Weifang Medical University, Weifang, Shandong, China. Electronic address: yanfang303@163.com.
  • 5 Department of Medicinal Chemistry, School of Pharmacy, Weifang Medical University, Weifang, Shandong, China. Electronic address: leiqdu@foxmail.com.
PMID: 32679451 DOI: 10.1016/j.ejmech.2020.112628
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.

Keywords

Histone deacetylase inhibitor; Physicochemical property; Prodrug; Selectivity; Structural modification.

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