Synthesis and biological activity of diisothiocyanate-derived mercapturic acids
| Autor: | Łukasz Winiarski, Agata Rudnicka, Renata Grzywa, Mateusz Psurski, Józef Oleksyszyn, Joanna Wietrzyk, Tadeusz Gajda |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
0301 basic medicine
Stereochemistry Colon Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Isothiocyanates Cell Line Tumor Drug Discovery Humans Mercapturic acid Molecular Biology Cell Proliferation Cell growth Chemistry Organic Chemistry Biological activity Acetylcysteine 030104 developmental biology Cell culture 030220 oncology & carcinogenesis Isothiocyanate Colonic Neoplasms Molecular Medicine Histone deacetylase activity Histone deacetylase Conjugate |
| Zdroj: | Bioorganicmedicinal chemistry letters. 26(2) |
| ISSN: | 1464-3405 |
| Popis: | This Letter deals with new non-natural diisothiocyanates, their mercapturic acid derivatives-conjugated with N-acetylcysteine as well as their antiproliferative activity towards human colon cancer cell lines and their inhibitory potency towards histone deacetylase activity. The activity of analysed isothiocyanates is not significantly different than their N-acetylcysteine conjugates. In comparison to simple mono-isothiocyanate analogues, aliphatic diisothiocyanates and their conjugates are much more active than the simple presence of two isothiocyanate functionalities could indicate. |
| Databáze: | OpenAIRE |
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