Investigating the in vitro Antitumor Structure-activity Relationship of a Range of Cannabinolic Acid Derivatives

Abstract

Aim: To investigate the in vitro structure-activity relationship (SAR) of a range of tetrahydrocannabinolic (THCA) and cannabidiolic (CBDA) derivatives using the PANC-1 tumor cell line (pancreas, ductal carcinoma). Materials and methods: The in vitro effects of a range of THCA and CBDA derivatives with different carbonyl group substituents were tested on the PANC-1 cells cell line using the CellTiter Glo Viability Assay (72 hours) and the XTT assay (48 hours). Results: A study of a series of THCA and CBDA derivatives containing different functional groups at the carbonyl nitrogen atom demonstrated that THCA amides have better inhibitory activity, on the PANC-1 tumor cell line, than CBDA derivatives. Conclusions: THCA derivatives have better inhibitory activity than CBDA analogs with the same substituents. It is noteworthy that even a slight change in the structure of the substituent of the amide or hydrazone moiety of the molecule has a dramatic effect on the activity of these compounds.