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Thesis . 2022
License: CC BY
Data sources: Datacite
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ZENODO
Thesis . 2022
License: CC BY
Data sources: Datacite
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DIARYL BIOLOGICALLY ACTIVE COMPOUNDS: POTENTIAL TREATMENTS FOR PARASITIC DISEASES AND CANCER AND NOVEL SYNTHETIC METHODS

Authors: Hicken, Ryan;

DIARYL BIOLOGICALLY ACTIVE COMPOUNDS: POTENTIAL TREATMENTS FOR PARASITIC DISEASES AND CANCER AND NOVEL SYNTHETIC METHODS

Abstract

Diaryl compounds have inhibitory activity towards multiple parasites and forms of cancer. In this study, new compounds have been synthesized to investigate their inhibitory activities towards Chagas Disease, which is caused by the parasite Trypanosoma cruzi and has infected millions of people in Latin America, causing health complications and in many cases death. Additionally, these compounds have been studied for AKT inhibition to inhibit the growth of cancerous cells. In this research, aryl substitutions, as well as the structural core, have been studied, producing compounds that are able to successfully inhibit the AKT pathway and T. cruzi epimastigote growth. In addition, the formation of these compounds was studied through the development of a flow reaction for the synthesis of 2-arylidene cycloalkanones, a key intermediate in the synthesis of asymmetric diarylidene cycloalkanones which exhibited strong inhibition towards AKT and T. cruzi. With this novel reaction, 2-arylidene cycloalkanones can be synthesized effectively. Additionally, this reaction was validated over 48 hours, and the scope was explored with a small library of starting materials. Through this new reaction, researchers can more efficiently synthesize 2-arylidene cycloalkanones to generate promising compounds for future investigations.

Keywords

flow chemistry, Chagas Disease, AKT inhibition

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selected citations
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This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
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