Synthesis and antitumor activity of benzophenone compound

Abstract

Seven benzophenone compounds were synthesized in one or two steps, then their antitumor activity was evaluated. The total yields ranged from 9% to 44%. Compounds 3c–5c exhibited obvious antitumor activity. Among them, compounds 3c and 4c exhibited excellent and broad-spectrum antitumor activity. Compound 3c exhibited much stronger inhibitory activities against fourteen cancer cells than cisplatin. In particular, compound 3c exhibited stronger cytotoxicity against hepatocarcinoma SMMC-7721 cells than Taxol, with a half maximal inhibitory concentration (IC₅₀) of approximately 0.111 μM. These results demonstrated that compounds 3c, 4c and 5c were very promising antitumor leads for further structural modification.

Graphical Abstract

Keywords:

• Synthesis
• benzophenone
• antitumor
• Eaton’s reagent

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) and Joint Special Project of Local Undergraduate Universities in Yunnan Province, China (Grant number 2018FH001-024) for the support of this program.