Ontology highlight
ABSTRACT:
SUBMITTER: Archer KE
PROVIDER: S-EPMC6691681 | biostudies-literature | 2019 Aug
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20190722 8
Indolinobenzodiazepine DNA alkylators (IGNs) are the cytotoxic payloads in antibody-drug conjugates (ADCs) currently undergoing Phase I clinical evaluation (IMGN779, IMGN632, and TAK164). These ADCs possess linkers that have been incorporated into a central substituted phenyl spacer. Here, we present an alternative strategy for the IGNs, linking through a carbamate at the readily available N-10 amine present in the monoimine containing dimer. As a result, we have designed a series of N-10 linked ...[more]