Sēru saturošo histonu deacetilāžu inhibitoru sintēzes metodes
Date
2006
Authors
Ruskovs, Dmitrijs
Journal Title
Journal ISSN
Volume Title
Publisher
Latvijas Universitāte
Abstract
Darbā apskatītas un salīdzinātas vairākas mūsdienās plaši lietotas sēru saturošo histonu deacetilāžu (HDAC) iespējamo inhibitoru sintēzes metodes. Uzmanība pievērsta tādiem savienojumiem kā tioli, -tiolketoni, tioesteri un -S-acil ketoni. Izklāstīta pēdējā laikā pieejamā informācija par HDAC inhibitoru iedarbību. Sintezēti 6 savienojumi ar iespējamo HDAC inhibējošo iedarbību un aprakstītas to īpašības. Vielu struktūra pierādīta ar PMR spektriem un elementanalīzi. Lietojot augsti efektīvo šķidruma - šķidruma hromatogrāfiju (AEŠH), tika noteikta vielu tīrība. Izstrādāta tiolu sudraba sāļu acilēšanas metode, kurai varētu būt praktiska nozīme līdzīgu savienojumu sintēzē.
In this work several common methods of possible sulfur containing histone deacetylase (HDAC) inhibitor synthesis are represented and compared. The main focus of the work are syntheses of thiols, -thiol ketones, -S-acyl ketones, thioesters. The latest information about the mechanism of HDAC inhibitor activity is given. 6 possible HDAC inhibitors were synthesized and their properties are described. The substances were identified by means of PMR spectra and elemental analyses. The purity of compounds were determined using high performance liquid chromatography (HPLC). A method of acylation of thiol silver salts, that could have a practical importance in synthesis of similar compounds, was elaborated.
In this work several common methods of possible sulfur containing histone deacetylase (HDAC) inhibitor synthesis are represented and compared. The main focus of the work are syntheses of thiols, -thiol ketones, -S-acyl ketones, thioesters. The latest information about the mechanism of HDAC inhibitor activity is given. 6 possible HDAC inhibitors were synthesized and their properties are described. The substances were identified by means of PMR spectra and elemental analyses. The purity of compounds were determined using high performance liquid chromatography (HPLC). A method of acylation of thiol silver salts, that could have a practical importance in synthesis of similar compounds, was elaborated.
Description
Keywords
Ķīmija