Anticancer Activity of Resorcinarene-PAMAM-Dendrimer Conjugates of Flutamide

Author(s): Luis D. Pedro-Hernández, Elena Martínez-Klimova*, Mark E. Martínez-Klimov, Sandra Cortez-Maya, Ana C. Vargas-Medina, Teresa Ramírez-Ápan, Simón Hernández-Ortega, Marcos Martínez-García

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 18 , Issue 7 , 2018

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Graphical Abstract:


Methods: The synthesis of conjugates of flutamide with resorcinarene-PAMAM-dendrimers as well as alkyl and ethyl phenyl chains in the lower part of the macrocycle as a nucleus and diethylenetriamines in the dendritic branches gives the opportunity to obtain conjugates in one step of synthesis with 16 and 64 flutamide moieties in the structure.

Results: The in vitro anticancer studies showed that the conjugates of flutamide are more active than the free flutamide and the flutamide derivatives, thus diminishing the amount of flutamide used. The resorcinarenedendrimer- flutamide conjugates with a high drug payload improve the activity of the drug.

Conclusion: This is important in delivering a sufficient amount of flutamide and suggests that the dendrimer facilitates more of the drug being introduced into cells. It was also observed that the new conjugates are less toxic than the anti-androgens.

Keywords: Dendrimers, conjugates, flutamide, anticancer, apoptosis, anti-androgens.

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Article Details

Year: 2018
Published on: 18 December, 2017
Page: [993 - 1000]
Pages: 8
DOI: 10.2174/1871520618666171219114532
Price: $65

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