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Updated: Mar 6, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Diversity-oriented synthesis and cytotoxic activity evaluation of biaryl-containing macrocycles
Karell Pérez-Labrada1, Marco A Cruz-Mendoza, Alejandra Chávez-Riveros
1Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior S.N., Ciudad Universitaria, Coyoacán, Ciudad de México, 04510, Mexico. lmiranda@unam.mx.
Abstract:
Synthesis of biaryl-containing macrocycles has been carried out through a four-step approach comprising two Ugi four component reactions and a Suzuki-Miyaura macrocyclization. This protocol allowed the synthesis of 12- and 14-membered macrocycles. Cytotoxic activity evaluation showed that some of the molecules were effective against leukemia, glioblastoma and lung cancer cell lines (IC50 = 4.0, 5.9 and 7.6, respectively).

