Identification of selenocompounds with promising properties to reverse cancer multidrug resistance

Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line

“…Subfamily B Member 1) protein in MDR mouse T-lymphoma cells as shown previously 25 ; as well as their capacity to trigger apoptotic events in these mouse Tlymphoma cells 25 . Results showed a noteworthy and promising activity, as the four most active compounds (1, 9-11, Figure 1) exerted a (1.7-3.6)-fold stronger efflux pump inhibitory activity than the reference verapamil at concentration 10-fold lower.…”

“…Results showed a noteworthy and promising activity, as the four most active compounds (1, 9-11, Figure 1) exerted a (1.7-3.6)-fold stronger efflux pump inhibitory activity than the reference verapamil at concentration 10-fold lower. In addition, those four most active selenium derivatives triggered apoptotic events in more than the 80% of the gated cells 25 .…”

“…The aim of our study is to compare the MDR reversing and efflux pump inhibiting properties of selenocompounds 1-11 in human cancer cell lines with the previous results in mouse cells 25 , as well as to evaluate their cytotoxicity in normal cells to determine their selectivity. For comparison, four additional compounds have been chosen as references to estimate the role of the presence of a selenium atom ( Table 1).…”

“…In this study we evaluate a series of the selenocompounds previously reported 20,21 that showed activity 25 as novel efflux pump inhibitors in parental L5178Y mouse T-lymphoma cells and in its MDR subline that expresses the ABCB1 protein after being transfected with the human ABCB1 gene 35 . Thus, the selenocarbonyl compounds 1-11, shown in Table 1, have been examined in different biological studies at the ABCB1-overexpressing Colo 320/MDR-LRP resistant cell line, as well as the equivalent sensitive cell line (Colo 205 doxorubicin sensitive cells), following previously described methodologies 25,27,[34][35][36][37][38] .…”

“…Thus, the selenocarbonyl compounds 1-11, shown in Table 1, have been examined in different biological studies at the ABCB1-overexpressing Colo 320/MDR-LRP resistant cell line, as well as the equivalent sensitive cell line (Colo 205 doxorubicin sensitive cells), following previously described methodologies 25,27,[34][35][36][37][38] . The selected derivatives 1-11 included the selenoanhydride 1 and the selenoesters 2-11, whose alkyl moiety contains different functional groups: a methyl group in 2-5, a methylcarbamoil group in 6, a methyloxycarbonylmethyl group in 7, a phenyloxycarbonylmethyl group in 8 and different ketonecontaining alkyl groups in 9-11.…”