Pyridine Derivative

14,000,000 Leading Edge Experts on the ideXlab platform

Scan Science and Technology

Contact Leading Edge Experts & Companies

Scan Science and Technology

Contact Leading Edge Experts & Companies

The Experts below are selected from a list of 6258 Experts worldwide ranked by ideXlab platform

Osamu Uchikawa - One of the best experts on this subject based on the ideXlab platform.

Yasutaka Hoashi - One of the best experts on this subject based on the ideXlab platform.

Tatsuki Koike - One of the best experts on this subject based on the ideXlab platform.

Takafumi Takai - One of the best experts on this subject based on the ideXlab platform.

Paola Gratteri - One of the best experts on this subject based on the ideXlab platform.

  • Pyridine Derivative of the natural alkaloid berberine as human telomeric g4 dna binder a solution and solid state study
    ACS Medicinal Chemistry Letters, 2020
    Co-Authors: Francesco Papi, Paolo Lombardi, Carla Bazzicalupi, M Ferraroni, Giulia Ciolli, Asma Yasmeen Khan, Gopinatha Suresh Kumar, Paola Gratteri
    Abstract:

    Telomerase is an enzyme deputed to the maintenance of eukaryotic chromosomes; however, its overexpression is a recognized hallmark of many cancer forms. A viable route for the inhibition of telomerase in malignant cells is the stabilization of G-quadruplex structures (G4) at the 3′ overhang of telomeres. Berberine has shown in this regard valuable G4 binding properties together with a significant anticancer activity and telomerase inhibition effects. Here, we focused on a berberine Derivative featuring a Pyridine containing side group at the 13th position. Such modification actually improves the binding toward telomeric G-quadruplexes and establishes a degree of selectivity in the interaction with different sequences. Moreover, the X-ray crystal structure obtained for the complex formed by the ligand and a bimolecular human telomeric quadruplex affords a better understanding of the 13-berberine Derivatives behavior with telomeric G4 and allows to draw useful insights for the future design of Derivatives w...

  • Pyridine Derivative of the natural alkaloid berberine as human telomeric g4 dna binder a solution and solid state study
    ACS Medicinal Chemistry Letters, 2020
    Co-Authors: Francesco Papi, Paolo Lombardi, Carla Bazzicalupi, M Ferraroni, Giulia Ciolli, Asma Yasmeen Khan, Gopinatha Suresh Kumar, Paola Gratteri
    Abstract:

    Telomerase is an enzyme deputed to the maintenance of eukaryotic chromosomes; however, its overexpression is a recognized hallmark of many cancer forms. A viable route for the inhibition of telomerase in malignant cells is the stabilization of G-quadruplex structures (G4) at the 3' overhang of telomeres. Berberine has shown in this regard valuable G4 binding properties together with a significant anticancer activity and telomerase inhibition effects. Here, we focused on a berberine Derivative featuring a Pyridine containing side group at the 13th position. Such modification actually improves the binding toward telomeric G-quadruplexes and establishes a degree of selectivity in the interaction with different sequences. Moreover, the X-ray crystal structure obtained for the complex formed by the ligand and a bimolecular human telomeric quadruplex affords a better understanding of the 13-berberine Derivatives behavior with telomeric G4 and allows to draw useful insights for the future design of Derivatives with remarkable anticancer properties.