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).Ma...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.展开更多
文摘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.
