The X-ray structure of a dendrimeric receptor based on calixarenes showed a packed periphery in the first generation. The presence of urea groups as linkers between the calix[4]arene core and the calix[6]arene dendrons makes it a good model as an endo-receptor which is able to coordinate squarate dianions with a high association constant.
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Bioorg Chem
September 2023
Department of Chemistry, Life Sciences and Environmental Sustainability, Parco Area delle Scienze 17/a, 43124 Parma, Italy. Electronic address:
We report the synthesis and biological characterization of a novel class of multivalent glycoconjugates as hit compounds for the design of new antiadhesive therapies against urogenital tract infections (UTIs) caused by uropathogenic E. coli strains (UPEC). The first step of UTIs is the molecular recognition of high mannose N-glycan expressed on the surface of urothelial cells by the bacterial lectin FimH, allowing the pathogen adhesion required for mammalian cell invasion.
View Article and Find Full Text PDFEur J Med Chem
February 2022
Instituto de Investigaciones en Materiales, Universidad Nacional Autónoma de México, Mexico City, 04510, Mexico. Electronic address:
Nanomedicine is an emerging area that largely influences the efficacy of various therapies through the rational design of new materials exhibiting more targeted behavior. The synthetic effort, the amount of used material, and the cost are critical parameters to bear in mind if the production of the designed material is intended to be scaled for their widespread use. Even though materials science offers diverse options for different types of therapies, it is a difficult task to meet all the parameters mentioned above.
View Article and Find Full Text PDFJ Med Chem
October 2021
Department of Chemistry, Laboratory of Bio-Organic Chemistry - NAmur Research Institute for LIfe Sciences (NARILIS), University of Namur (UNamur), Rue de Bruxelles 61, 5000 Namur, Belgium.
(P.A.) is a human pathogen belonging to the top priorities for the discovery of new therapeutic solutions.
View Article and Find Full Text PDFMolecules
April 2021
Laboratoire de Chimie des Matériaux Moléculaires, Université de Strasbourg et CNRS (UMR 7402 LIMA), Ecole Européenne de Chimie, Polymères et Matériaux, 25 rue Becquerel, CEDEX 2, 67087 Strasbourg, France.
With their ten peripheral substituents, pillar[5]arenes are attractive compact scaffolds for the construction of nanomaterials with a controlled number of functional groups distributed around the macrocyclic core. This review paper is focused on the functionalization of pillar[5]arene derivatives with small dendrons to generate dendrimer-like nanomaterials and bioactive compounds. Examples include non-viral gene vectors, bioactive glycoclusters, and liquid-crystalline materials.
View Article and Find Full Text PDFBioorg Med Chem Lett
July 2020
Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Exterior, Coyoacán, C.P 04510 México, D.F., Mexico. Electronic address:
The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells.
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