TY - JOUR
T1 - Synthesis and antiproliferative activity of novel steroidal dendrimer conjugates
AU - Magaña-Vergara, Nancy E.
AU - Rárová, Lucie
AU - Soto-Castro, Delia
AU - Farfán, Norberto
AU - Strnad, Miroslav
AU - Santillan, Rosa
N1 - Funding Information:
The authors thank ICyT for the scholarship to N.-E. Magaña-Vergara. Thanks are given to Ma. T. Cortez for NMR spectra, G. Cuéllar for mass spectra and Prof. Igor Alabugin for his suggestions and critical reading of the manuscript. The Ministry of Education, Youth and Sports of the Czech Republic (grant No. MSM 6198959216 ) and the Centre of the Region Haná for Biotechnological and Agricultural Research (grant No. ED0007/01/01 ). Financial support from CONACYT is gratefully acknowledged.
PY - 2013
Y1 - 2013
N2 - We describe the synthesis of steroidal dendrimer conjugates of first and second generation with tetramethylene core and 5-hydroxy-isophtalic acid dimethyl ester as branching unit modified to incorporate ethynylestradiol or 17α-estradiol as terminal units. The steroidal dendrimer conjugates, the free drug (steroids) and dendrimer were tested against a panel of cancer cell lines (CEM, MCF7, HeLa) and normal human fibroblast (BJ). The steroidal dendrimer conjugates of first generation exhibited cytotoxic activity and induced apoptosis in chronic leukemia (CEM) as resultant activation of caspase cascade which is mainly provoked in G2/M arrested cells.
AB - We describe the synthesis of steroidal dendrimer conjugates of first and second generation with tetramethylene core and 5-hydroxy-isophtalic acid dimethyl ester as branching unit modified to incorporate ethynylestradiol or 17α-estradiol as terminal units. The steroidal dendrimer conjugates, the free drug (steroids) and dendrimer were tested against a panel of cancer cell lines (CEM, MCF7, HeLa) and normal human fibroblast (BJ). The steroidal dendrimer conjugates of first generation exhibited cytotoxic activity and induced apoptosis in chronic leukemia (CEM) as resultant activation of caspase cascade which is mainly provoked in G2/M arrested cells.
KW - Antiproliferative activity
KW - Ethynylestradiol
KW - Steroidal dendrimer conjugates
UR - http://www.scopus.com/inward/record.url?scp=84884920039&partnerID=8YFLogxK
U2 - 10.1016/j.steroids.2013.09.001
DO - 10.1016/j.steroids.2013.09.001
M3 - Artículo
SN - 0039-128X
VL - 78
SP - 1254
EP - 1262
JO - Steroids
JF - Steroids
IS - 12-13
ER -