TY - JOUR
T1 - Synthesis and structure-activity relationships of novel ecdysteroid dioxolanes as MDR modulators in cancer.
AU - Amaral, Leonard
AU - Martins, Ana
PY - 2013/1/1
Y1 - 2013/1/1
N2 - Ecdysteroids, molting hormones of insects, can exert several mild, non-hormonal bioactivities in mammals, including humans. In a previous study, we have found a significant effect of certain derivatives on the ABCB1 transporter mediated multi-drug resistance of a transfected murine leukemia cell line. In this paper, we present a structure-activity relationship study focused on the apolar dioxolane derivatives of 20-hydroxyecdysone. Semi-synthesis and bioactivity of a total of 32 ecdysteroids, including 20 new compounds, is presented, supplemented with their complete 1H- and 13C-NMR signal assignment.
AB - Ecdysteroids, molting hormones of insects, can exert several mild, non-hormonal bioactivities in mammals, including humans. In a previous study, we have found a significant effect of certain derivatives on the ABCB1 transporter mediated multi-drug resistance of a transfected murine leukemia cell line. In this paper, we present a structure-activity relationship study focused on the apolar dioxolane derivatives of 20-hydroxyecdysone. Semi-synthesis and bioactivity of a total of 32 ecdysteroids, including 20 new compounds, is presented, supplemented with their complete 1H- and 13C-NMR signal assignment.
U2 - 10.3390/molecules181215255
DO - 10.3390/molecules181215255
M3 - Article
C2 - 24335576
VL - 18
SP - 15255
EP - 15275
JO - Molecules (Basel, Switzerland)
JF - Molecules (Basel, Switzerland)
SN - 1420-3049
IS - 12
ER -