Synthesis and Evaluation of C15 Triene Urushiol Derivatives as Potential Anticancer Agents and HDAC2 Inhibitor

A series of C15 triene urushiol derivatives were synthesized and evaluated for their anti-HepG2 aggregation in vitro. The results indicated that all compounds had an effective anti-HepG2 vitality. Compound 1 was a potent inhibitor of HepG2 with IC(50) of 7.886 μM and 150 μM against LO2. Moreover, co...

Descripción completa

Detalles Bibliográficos
Autores principales: Qi, Zhiwen, Wang, Chengzhang, Jiang, Jianxin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6102549/
https://www.ncbi.nlm.nih.gov/pubmed/29751548
http://dx.doi.org/10.3390/molecules23051074
Descripción
Sumario:A series of C15 triene urushiol derivatives were synthesized and evaluated for their anti-HepG2 aggregation in vitro. The results indicated that all compounds had an effective anti-HepG2 vitality. Compound 1 was a potent inhibitor of HepG2 with IC(50) of 7.886 μM and 150 μM against LO2. Moreover, compound 1 increased the apoptosis of HepG2. Compound 1’s thiol sulfur formed hydrogen bonding interactions with Gly154 and Tyr308, respectively, and made it bound more closely to HDAC2. In addition, it also formed hydrophobic interactions with the residues His33, Pro106, Val107, Gly154, Phe155, and His183, and was provided with a strong van der Waals force by the hydrophobic action.

Ejemplares similares