On-DNA Platform Molecules Based on a Diazide Scaffold II: A Compact Diazide Platform Designed for Small-Molecule Drug Discovery.

ABSTRACT: Expanding the chemical diversity of DNA-encoded libraries (DELs) is crucial for identifying binders to emerging drug targets using DEL technology. In the present study, as part of our ongoing efforts to develop on-DNA diazide platforms (D-DAPs)-platform molecules possessing both aromatic and aliphatic azide groups on a single core reactive scaffold-we designed and synthesized a new compact diazide platform, designated as a compact D-DAP (C-D-DAP). This molecule is based on a low-molecular-weight reactive scaffold, 3-azido-5-(azidomethyl)benzoic acid, to facilitate small-molecule drug discovery targeting enzymes and G protein-coupled receptors (GPCRs). Furthermore, we established two distinct stepwise warhead construction strategies that exploit the chemoselective transformations of the azi

SUBMITTER: Miyachi H 

PROVIDER: S-EPMC12841052 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature