Title:Anticancer Activity of Resorcinarene-PAMAM-Dendrimer Conjugates of Flutamide
VOLUME: 18 ISSUE: 7
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 and Marcos Martínez-García
Affiliation:Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Fisiologia Celular, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F, Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Circuito Exterior, Coyoacan, C.P. 04510, Mexico D.F
Keywords:Dendrimers, conjugates, flutamide, anticancer, apoptosis, anti-androgens.
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.
