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

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.

In vitro Activity of Novel Cannabinoids Derived from Tetrahydrocan-nabinolic Acid on Various Human Tumor Cell Lines

The in vitro study of tetracannabinolic acid(THCA)derivatives ALAM027 and ALAM108 was carried out on the following human tumor cells:T47D(breast,ductal carcinoma),PC-3(prostate,adenocarcinoma),HT 29(colorectal carcinoma),Caco-2(colon,adenocarcinoma),A549(lung,carcinoma),U87MG(human glioblastoma)and U266B1(multiple myeloma).The in vitro effects of THCA derivatives ALAM027 and ALAM108 on cell growth inhibition and IC50 values were measured using the CellTiter Glo assay.The ALAM027 compound showed good growth inhibition in all cell lines tested with the exception of U87MG cells.The ALAM108 compound also suppressed the growth of U87 MG cells but had little effect on T47D tumor cells.In vitro studies of THCA derivatives ALAM027 and ALAM108 showed antitumor activity in all cell lines tested.The difference in the activity of these compounds in relation to the T47D and U87MG tumor cells may be indicative of different functional mechanisms.