Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01563
Abstract: G-quadruplex stabilizers are an established opportunity in anticancer chemotherapy. To circumvent the antiproliferative effects of G4 ligands, cancer cells recruit PARP enzymes at telomeres. Herein, starting from the structural similarity of a potent G4 ligand… read more here.
Keywords: dual quadruplex; discovery dual; stabilizers poly; quadruplex stabilizers ... See more keywords
Pursuing Polypharmacology: Benzothiopyranoindoles as G-Quadruplex Stabilizers and Topoisomerase I Inhibitors for Effective Anticancer Strategies.
Sign Up to like & getrecommendations! Published in 2024 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.4c00313
Abstract: Here, we explored the benzothiopyranoindole scaffold to develop antiproliferative agents with a polypharmacological profile targeting both G-quadruplex (G4)-structures and Topoisomerase (Topo) I enzyme. In a preliminary optimization phase, compound 1 was selected from an in-house… read more here.
Keywords: polypharmacology benzothiopyranoindoles; pursuing polypharmacology; anticancer; quadruplex stabilizers ... See more keywords