Reactivity Modulation of Reactive OFF-ON Type G-Quadruplex Alkylating Agents.
Journal
Bioconjugate chemistry
ISSN: 1520-4812
Titre abrégé: Bioconjug Chem
Pays: United States
ID NLM: 9010319
Informations de publication
Date de publication:
16 11 2022
16 11 2022
Historique:
pubmed:
1
11
2022
medline:
19
11
2022
entrez:
31
10
2022
Statut:
ppublish
Résumé
Alkylating agents for nucleic acids have been widely used in cancer chemotherapy, as well as in chemical biology for strong inhibitors and tagging methods. We provide a series of reactive OFF-ON type alkylating agents which enable the reactivity modulation toward G-quadruplex (G4) DNA and RNA. Due to the protonation-accelerated process and equilibrium elimination method, the amine leaving groups show highly reactive and storable properties in an extensive investigation of vinyl quinazolinone (VQ) precursors with different leaving groups.
Identifiants
pubmed: 36315583
doi: 10.1021/acs.bioconjchem.2c00458
doi:
Substances chimiques
Alkylating Agents
0
DNA
9007-49-2
RNA
63231-63-0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM