Multicomponent synthesis and anti-proliferative screening of biaryl triazole-containing cyclophanes.
Basic Information
ID: ALA4813986
Journal: Bioorg Med Chem Lett
Title: Multicomponent synthesis and anti-proliferative screening of biaryl triazole-containing cyclophanes.
Authors: Hernández-Vázquez E, Amador-Sánchez YA, Cruz-Mendoza MA, Ramírez-Apán MT, Miranda LD.
Abstract: We report a practical two-step approach involving a Ugi 4-CR/ azide-alkyne cycloaddition for the synthesis of biaryl-containing cyclophanes. The series represents an extension of our previously reported macrocycles as an effort to enhance the anti-proliferative activity of this scaffold. In this variant, we incorporate a biphenyl moiety in the framework, thus enhancing the macrocycle size, lipophilicity, and structural diversity. Macrocycles were tested against different cell lines, being more cytotoxic against prostate (PC-3 and DU-145) and breast (MCF-7) tumor cells. Gratifyingly, the most active compound showed a significative enhancement of PC-3 growth inhibition with respect to our previous series, reaffirming the potential anti-proliferative activity of this kind of cyclophanes.
CiteXplore: 33722739
DOI: 10.1016/j.bmcl.2021.127899
Patent ID: ┄