Synthesis of Heteroaromatic Cycle Containing Histone Deacetylase Inhibitors and Their Structure – Activity Relationships
2010
Olga Habarova

Supervisor
Einārs Loža

Reviewers
Andris Strakovs, Peteris Trapencieris, Arkadijs Soboļevs

Theses focuses on the research of histone deacetylase inhibitors containing quinoline cycle. Methodology of the synthesis of hydroxamic acids from esters in the presence of sodium ethylate was developed. Methodology of the synthesis of (E)-N-hydroxy-3-quinolinylacrylamide and their derivatives was developed. Methodology of the (E)-N-hydroxy-3-quinolin-2-yl acryric acid amidation was developed. (E)-1,1,1-Trifluoro-6-quinolin-2-ylhex-5-ene-2,4-dione structure and its keto-enol forms transformations has been investigated. Methodology of the synthesis of thioacetic acid S-((E)-2-oxo-4-quinolin-2-ylbut-3-enyl) ester derivatives was developed. Methodology of the synthesis of (E)-2-quinolin-2-yl-ethenesulfonic acid (1,1,3,3-tetramethylbutyl)amide via Heck reaction was investigated. Representatives of the new types of quinoline-2-carbonic acid pentylamide derivatives - potentially histone deacetylases inhibitors were synthesized.


Keywords
HISTONE DEACETYLASE, INHIBITORS OF HISTONE DEACETYLASE, QUINOLINE, Zn2+ CHELATING GROUPS, HYDROXAMIC ACID, SKRAUP REACTION, HORNER-WADSWORTH-EMMONS REACTION, AMIDATION OF CARBOXYLIC ACIDS, AMINOBENZOAMIDES, S-2-OXOETHYLTHIOATES, HECK REACTION

Habarova, Olga. Synthesis of Heteroaromatic Cycle Containing Histone Deacetylase Inhibitors and Their Structure – Activity Relationships. PhD Thesis. Rīga: [RTU], 2010. 157 p.

Publication language
Latvian (lv)
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