Ontology highlight
ABSTRACT:
SUBMITTER: Zaware N
PROVIDER: S-EPMC5398096 | biostudies-literature | 2017 Apr
REPOSITORIES: biostudies-literature
Zaware Nilesh N Kisliuk Roy R Bastian Anja A Ihnat Michael A MA Gangjee Aleem A
Bioorganic & medicinal chemistry letters 20170211 7
In an effort to optimize the structural requirements for combined cytostatic and cytotoxic effects in single agents, a series of 5-(arylthio)-9H-pyrimido[4,5-b]indole-2,4-diamines 3-7 were synthesized and evaluated as inhibitors of receptor tyrosine kinases (RTKs) as well as thymidylate synthase (TS). The synthesis of these compounds involved the nucleophilic displacement of the common intermediate 5-bromo/5-chloro-9H-pyrimido[4,5-b]indole-2,4-diamine with appropriate aryl thiols. A novel four s ...[more]