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

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...

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Bibliographic Details
Main Author: Green, Julius
Format: Others
Published: ScholarWorks @ Georgia State University 2014
Subjects:
Combilexin
Diazaborole
DNA minor groove binder
African Sleeping Sickness
Online Access:http://scholarworks.gsu.edu/chemistry_diss/101
http://scholarworks.gsu.edu/cgi/viewcontent.cgi?article=1106&context=chemistry_diss
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spelling ndltd-GEORGIA-oai-scholarworks.gsu.edu-chemistry_diss-11062014-08-28T03:37:59Z Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents Green, Julius 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. 2014-12-17T08:00:00Z text application/pdf http://scholarworks.gsu.edu/chemistry_diss/101 http://scholarworks.gsu.edu/cgi/viewcontent.cgi?article=1106&context=chemistry_diss Chemistry Dissertations ScholarWorks @ Georgia State University Combilexin Diazaborole DNA minor groove binder African Sleeping Sickness
collection NDLTD
format Others
sources NDLTD
topic Combilexin
Diazaborole
DNA minor groove binder
African Sleeping Sickness
spellingShingle Combilexin
Diazaborole
DNA minor groove binder
African Sleeping Sickness
Green, Julius
Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
description 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.
author Green, Julius
author_facet Green, Julius
author_sort Green, Julius
title Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
title_short Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
title_full Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
title_fullStr Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
title_full_unstemmed Synthesis of Aza-Heterocyclic Monoamidines as Potential DNA Minor Groove Binders, Anti-Trypanosomals, and Boron Neutron Capture Therapy Agents
title_sort synthesis of aza-heterocyclic monoamidines as potential dna minor groove binders, anti-trypanosomals, and boron neutron capture therapy agents
publisher ScholarWorks @ Georgia State University
publishDate 2014
url http://scholarworks.gsu.edu/chemistry_diss/101
http://scholarworks.gsu.edu/cgi/viewcontent.cgi?article=1106&context=chemistry_diss
work_keys_str_mv AT greenjulius synthesisofazaheterocyclicmonoamidinesaspotentialdnaminorgroovebindersantitrypanosomalsandboronneutroncapturetherapyagents
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