Synthesis and in vitro antiproliferative evaluation of some ring B abeo-sterols
| Autor: | Lianghua Fan, Wanxin Wei, Yanmin Huang, Jianguo Cui, Chunfang Gan, Jiao Yanxiao |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Thiosemicarbazones
Cell Survival Stereochemistry Clinical Biochemistry Antineoplastic Agents Biochemistry HeLa Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Endocrinology Cell Line Tumor medicine Side chain Humans Cytotoxic T cell Cytotoxicity Molecular Biology Semicarbazone Pharmacology Cisplatin biology Organic Chemistry Dehydroepiandrosterone biology.organism_classification Sitosterols In vitro Sterols Cholesterol chemistry Pregnenolone Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | Steroids. 77:1061-1068 |
| ISSN: | 0039-128X |
| DOI: | 10.1016/j.steroids.2012.05.005 |
| Popis: | Using cholesterol, β-sitosterol, dehydroisoandrosterone and pregnenolone as starting materials, a series of 5(6 → 7)abeo-sterols with different substituted groups and various side chains were synthesized and the antiproliferative activity of these compounds against HeLa, SMMC 7404 and MGC 7901 cells was investigated. The results revealed that the presence of a cholesterol-type side chain was very important for their cytotoxicity, and in particular a thiosemicarbazone at the C-6 position significantly enhanced the antiproliferative activity of these compounds. Although the elimination of 5-hydroxyl has no an obvious effect on their cytotoxic function, removal of the hydroxyl at the C-3 position decreased markedly the antiproliferative activity of the compounds. Some compounds have similar cytotoxic capability as cisplatin does. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect