Synthesis and antiproliferative activity of CBD aromatic ester derivatives

Abstract

This study involved the synthesis of a series of novel cannabidiol (CBD) aromatic ester derivatives, including CBD-8,12-diaromaticester derivatives (compounds 2a–2t) and CBD-8,12-diacetyl-21-aromaticester derivatives (compound 5a–5c). The antiproliferative activities of these compounds against human liver cancer cell lines HePG2 and HeP3B as well as human pancreatic cancer cell lines ASPC-1 and BXPC-3 were evaluated in vitro using the CCK-8 assay. The results indicated that compound 2f exhibited an IC₅₀ value of 2.75 µM against HePG2, which is 5.32-fold higher than that of CBD. Additionally, compounds 2b and 5b demonstrated varying degrees of improved anticancer activity (IC₅₀ 5.95-9.21 µM) against HePG2.

GRAPHIC ABSTRACT

Keywords:

• CBD
• CBD aromatic ester derivatives
• anticancer activity

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research was financially supported by National Key Research and Development Program (2022YFD1801103) and Natural Science Foundation of Hunan Province (2022JJ30283).