Efficient synthesis, and antitumor and antioxidant activities of polyhydroxybenzophenone

Abstract

Five polyhydroxybenzophenones were synthesized, then their antitumor and antioxidant activities were evaluated. Compounds 1–3 and 5 exhibited obvious antitumor activity. Among them, compounds 1 and 2 exhibited stronger cytotoxicity against hepatocarcinoma SMMC-7721 cells than cisplatin, with half maximal inhibitory concentrations (IC₅₀) of approximately 3.86 and 5.32 μM, respectively. Compounds 1, 2, and 3 exhibited stronger antioxidant activity than trolox, with IC₅₀ values of 11.15, 10.15, and 8.91 μM, respectively, and the antioxidant mechanism and strength of all compounds were further verified using computational chemistry. These results demonstrated that compounds 1–3 and 5 were very promising leads for further structural modification.

Graphical abstract

Keywords:

• Synthesis
• benzophenone
• antitumor
• antioxidant
• computational chemistry

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

The authors gratefully thank the Leading Project of Fujian Provincial Department of Science and Technology (Grant number 2018Y0072), Fujian Provincial Key Laboratory of Innovative Drug Target Research (Grant number FJ-YW-2021KF01), the National Natural Science Foundation of China (Grant number 31960480), Joint Special Project of Local Undergraduate Universities in Yunnan Province, China (Grant number 2018FH001-024), and the Project of Yunnan Provincial Department of Education (Grant number 2019J0740) for the support of this program.