Convergent Synthesis of Symmetrical and Unsymmetrical PAMAM Dendrimers

2006 ◽  
Vol 39 (6) ◽  
pp. 2418-2422 ◽  
Author(s):  
Jae Wook Lee ◽  
Byung-Ku Kim ◽  
Hee Joo Kim ◽  
Seung Choul Han ◽  
Won Suk Shin ◽  
...  
2005 ◽  
Vol 7 (7) ◽  
pp. 1295-1298 ◽  
Author(s):  
Michael Pittelkow ◽  
Jørn B. Christensen

Tetrahedron ◽  
2006 ◽  
Vol 62 (39) ◽  
pp. 9193-9200 ◽  
Author(s):  
Jae Wook Lee ◽  
Jung Hwan Kim ◽  
Byung-Ku Kim ◽  
Ji Hyeon Kim ◽  
Won Suk Shin ◽  
...  

2012 ◽  
Vol 19 (29) ◽  
pp. 4969-4975 ◽  
Author(s):  
M. Goncalves ◽  
R. Castro ◽  
J. Rodrigues ◽  
H. Tomas

2015 ◽  
Vol 19 (19) ◽  
pp. 1954-1960 ◽  
Author(s):  
Sandra Cortez-Maya ◽  
Elena Klimova ◽  
R. I. Puente Lee ◽  
Andres Borja-Miranda ◽  
Marcos Martinez-Garcia

2020 ◽  
Vol 20 (15) ◽  
pp. 1857-1872
Author(s):  
Alberto M. Muñoz ◽  
Manuel J. Fragoso-Vázquez ◽  
Berenice P. Martel ◽  
Alma Chávez-Blanco ◽  
Alfonso Dueñas-González ◽  
...  

Background: Our research group has developed some Valproic Acid (VPA) derivatives employed as anti-proliferative compounds targeting the HDAC8 enzyme. However, some of these compounds are poorly soluble in water. Objective: Employed the four generations of Polyamidoamine (G4 PAMAM) dendrimers as drug carriers of these compounds to increase their water solubility for further in vitro evaluation. Methods: VPA derivatives were subjected to Docking and Molecular Dynamics (MD) simulations to evaluate their affinity on G4 PAMAM. Then, HPLC-UV/VIS, 1H NMR, MALDI-TOF and atomic force microscopy were employed to establish the formation of the drug-G4 PAMAM complexes. Results: The docking results showed that the amide groups of VPA derivatives make polar interactions with G4 PAMAM, whereas MD simulations corroborated the stability of the complexes. HPLC UV/VIS experiments showed an increase in the drug water solubility which was found to be directly proportional to the amount of G4 PAMAM. 1H NMR showed a disappearance of the proton amine group signals, correlating with docking results. MALDI-TOF and atomic force microscopy suggested the drug-G4 PAMAM dendrimer complexes formation. Discussion: In vitro studies showed that G4 PAMAM has toxicity in the micromolar concentration in MDAMB- 231, MCF7, and 3T3-L1 cell lines. VPA CF-G4 PAMAM dendrimer complex showed anti-proliferative properties in the micromolar concentration in MCF-7 and 3T3-L1, and in the milimolar concentration in MDAMB- 231, whereas VPA MF-G4 PAMAM dendrimer complex didn’t show effects on the three cell lines employed. Conclusion: These results demonstrate that G4 PAMAM dendrimers are capableof transporting poorly watersoluble aryl-VPA derivate compounds to increase its cytotoxic activity against neoplastic cell lines.


Sign in / Sign up

Export Citation Format

Share Document