Amides derived from heteroaromatic amines and selected steryl hemiesters
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
24145008
DOI
10.1016/j.steroids.2013.10.003
PII: S0039-128X(13)00217-1
Knihovny.cz E-zdroje
- Klíčová slova
- 4-(N,N-dimethylamino)pyridine, 50% solution of propylphosphonic anhydride in ethyl acetate, 9H-fluoren-9-ylmethyl carbonochloridate, Amide, BJ, CEM, Cholesterol, Cytotoxic activity, DCC, DMAP, DMEM, Dulbecco’s modified Eagle’s medium, FBS, FMOC-Cl, HeLa, Heteroaromatic amine, Lanosterol, MCF7, N,N′-dicyclohexylcarbodiimide, T3P, cells of human T-lymphoblastic leukemia, cells of human breast adenocarcinoma, cells of human cervical cancer, foetal bovine serum, normal human fibroblasts,
- MeSH
- amidy chemie MeSH
- aminy chemie MeSH
- cholesterol analogy a deriváty chemická syntéza farmakologie MeSH
- cytotoxiny chemická syntéza farmakologie MeSH
- fibroblasty cytologie účinky léků metabolismus MeSH
- lanosterol analogy a deriváty chemická syntéza farmakologie MeSH
- lidé MeSH
- magnetická rezonanční spektroskopie MeSH
- nádorové buněčné linie MeSH
- proliferace buněk účinky léků MeSH
- protinádorové látky chemická syntéza farmakologie MeSH
- screeningové testy protinádorových léčiv MeSH
- viabilita buněk účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- amidy MeSH
- aminy MeSH
- cholesterol MeSH
- cytotoxiny MeSH
- lanosterol MeSH
- protinádorové látky MeSH
The current interest of the team has been focused on investigation of novel amides with potential cytotoxicity. The presented series of compounds was synthesized from selected steryl hemiesters and heteroaromatic amines. The synthetic protocol was designed in a simple and economic way, and divided into several general methodologies applicable to the compounds synthesized. The cytotoxicity was tested on cells derived from human T-lymphoblastic leukemia, breast adenocarcinoma and cervical cancer, and compared with tests on normal human fibroblasts. Most of the lanosterol-based compounds (3-5 and 7-10) showed medium to good cytotoxicity, while only two derivatives of cholesterol (18 and 19) showed medium cytotoxicity on human T-lymphoblastic leukemia cell line. The compounds 8 and 9 displayed the reasonable cytotoxicity among this series of amides, tested on the cell lines of T-lymphoblastic leukemia [14.5±0.4 μM (8) and 18.5±3.9 μM (9)], breast adenocarcinoma [19.5±2.1 μM (8) and 23.1±4.0 μM (9)] and cervical cancer [24.8±5.3 μM (8) and 29.1±4.7 μM (9)]. Only the compound 8 was adequately less active on normal human fibroblasts (40.4±11.1 μM).
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