The effect of novel pectolinarigenin derivatives bearing a dialkylaminoalkyl substituent at O-7 on cellproliferation was evaluated in vitro in a panel of seven human cancer cell lines including renal adenocarcinomaACHN, amelanotic melanoma C32, colorectal adenocarcinoma Caco-2, lung large cell carcinomaCOR-L23, malignant melanoma A375, lung carcinoma A549 and hepatocellular carcinoma Huh-7D12 celllines. Pectolinarigenin (2), obtained by hydrolysis of rutinose unit of the pectolinarin (1) isolated fromLinaria reflexa, exhibited cytotoxic activity against Caco-2, A549 and A375 cell lines with IC50 values of5.3–8.2 microM. The most active pectolinarigenin derivative was 3 characterized by a dimethylamino-propoxygroup in O-7 with IC50 values of 7.2 and 7.4 microM against COR-L23 and A549 cell lines, respectively.A structure–activity relationship analysis of synthesized compounds was performed. None of the testedcompounds affected the proliferation of skin fibroblasts 142BR suggesting a selective activity againsttumor cells.
In vitro biological evaluation of novel 7-O-dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines
Bonesi M.;Tundis R.;Loizzo M. R.;
2008-01-01
Abstract
The effect of novel pectolinarigenin derivatives bearing a dialkylaminoalkyl substituent at O-7 on cellproliferation was evaluated in vitro in a panel of seven human cancer cell lines including renal adenocarcinomaACHN, amelanotic melanoma C32, colorectal adenocarcinoma Caco-2, lung large cell carcinomaCOR-L23, malignant melanoma A375, lung carcinoma A549 and hepatocellular carcinoma Huh-7D12 celllines. Pectolinarigenin (2), obtained by hydrolysis of rutinose unit of the pectolinarin (1) isolated fromLinaria reflexa, exhibited cytotoxic activity against Caco-2, A549 and A375 cell lines with IC50 values of5.3–8.2 microM. The most active pectolinarigenin derivative was 3 characterized by a dimethylamino-propoxygroup in O-7 with IC50 values of 7.2 and 7.4 microM against COR-L23 and A549 cell lines, respectively.A structure–activity relationship analysis of synthesized compounds was performed. None of the testedcompounds affected the proliferation of skin fibroblasts 142BR suggesting a selective activity againsttumor cells.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
