Synthesis and antiproliferative activity of novel steroidal dendrimer conjugates |
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| Authors: | Nancy E. Magaña-Vergara Lucie Rárová Delia Soto-Castro Norberto Farfán Miroslav Strnad Rosa Santillan |
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| Affiliation: | 1. Departamento de Química, Centro de Investigación y de Estudios Avanzados del IPN, Apdo. Postal 14-740, México D.F. 07000, Mexico;2. Centre of the Region Haná for Biotechnological and Agricultural Research, Faculty of Science, Palacký University, ?lechtitel? 11, CZ-783 71 Olomouc, Czech Republic;3. Facultad de Química, Departamento de Química Orgánica, Universidad Nacional Autónoma de México, México D.F. 04510, Mexico |
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| Abstract: | 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. |
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| Keywords: | Steroidal dendrimer conjugates Antiproliferative activity Ethynylestradiol |
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