Return to search

Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents

A series of combilexin-like monoamidines has been synthesized by linking an intercalative unit with the DNA minor groove binder DB 818 via “Click chemistry.” DB 818 is a dicationic minor groove binder that has shown strong binding affinity to AT sequences. The aim was to synthesize novel classes of DNA minor groove binders that are combilexin-like – minor groove binder / intercalator hybrid – as potential unique DNA binding agents and therapeutics against African Sleeping Sickness. Additionally, a series of novel benzo[d]1,3,2-diazaboroles DAPI derivatives were also synthesized and investigated. These boron compounds have the potential to be strong DNA minor groove binders because of their lower pKa and act as potential chromophores for Boron Neutron Capture Therapy.

Identiferoai:union.ndltd.org:GEORGIA/oai:scholarworks.gsu.edu:chemistry_diss-1106
Date17 December 2014
CreatorsGreen, Julius
PublisherScholarWorks @ Georgia State University
Source SetsGeorgia State University
Detected LanguageEnglish
Typetext
Formatapplication/pdf
SourceChemistry Dissertations

Page generated in 0.0019 seconds