Today, dendrimers are the main nanoparticle applied to drug delivery systems. The physicochemical characteristics of dendrimers and their versatility structural modification make them attractive to applied as a platform to bioactive molecules transport. Nanoformulations based on dendrimers enhance low solubility drugs, arrival to the target tissue, drugs bioavailability, and controlled release. This review describes the latter approaches on the transport of bioactive molecules based on dendrimers. The review focus is on the last therapeutic strategies addressed by dendrimers conjugated with bioactive molecules. A brief review of the latest studies in therapies against cancer and cardiovascular diseases, as well as future projections in the area, are addressed.
The relationship between ectopic neurotensin expression (NTS) and tumor carcinoma invasion has produced studies that point to allosteric modulation of the regular NTR1 receptor. The use of quinazoline-derived drugs has shown excellent results in the regulation of the biological process mentioned. This study aims to establish the relationship between the electronic structure of quinazoline derivatives and the biological activity (expressed as EC50) that process in the NTR1 receptor, to propose a 2D pharmacophore. For this purpose, the Klopman-Peradejordi-Gómez (KPG) methodology was used. Calculations are included within the functional density theory (DFT) using the B3LYP / 631G theory level (d, p). The results concerning the biological activity are mainly driven by the interactions at the orbitalorbital level and by charges. These results can be used to propose new quinazoline derivatives with a better response in allosteric modulation of the NTR1 receptor.
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