Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines
Jazyk angličtina Země Francie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
23981532
DOI
10.1016/j.ejmech.2013.08.009
PII: S0223-5234(13)00510-2
Knihovny.cz E-zdroje
- Klíčová slova
- 1-hydroxybenzotriazole hydrate, 5-bromo-2′-deoxyuridine, Apoptosis, Autophagy, B-cell lymphoma 2, B-cell lymphoma-extra large, Bcl-2, Bcl-xL, BrdU, CDK, Cancer, Cbz, Cytotoxicity, DCC, DCM, DMF, Diamides, EDC·HCl, ERK1/2, Et(2)O, Et(3)N, EtOAc, GSK, HMGB1, HOBt·H(2)O, IC(50), LC3, Mdm2, N,N′-dicyclohexylcarbodiimide, N,N′-dimethylformamide, N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, PARP-1, PET, RT, Rb, SAR, benzyloxycarbonyl group, cyclin-dependent kinase, dichloromethane, diethylether, ethyl acetate, extracellular-signal-regulated kinases, glycogen synthase kinase, growth inhibition 50%, high-mobility group protein B1, microtubule-associated protein light chain 3, mouse double minute 2, p53, photosynthetic electron transport, poly-(ADP-ribose)polymerase-1, retinoblastoma protein, room temperature (approx. 20 °C), structure–activity relationship, triethyl amine,
- MeSH
- apoptóza účinky léků MeSH
- benzamidy chemická syntéza chemie farmakologie MeSH
- buněčný cyklus účinky léků MeSH
- inhibiční koncentrace 50 MeSH
- lidé MeSH
- molekulární struktura MeSH
- nádorové buněčné linie MeSH
- protinádorové látky chemická syntéza chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- benzamide MeSH Prohlížeč
- benzamidy MeSH
- N-(1-(4-chlorophenyl)-3-(dimethylamino)propyl)-4-phenylbenzamide MeSH Prohlížeč
- protinádorové látky MeSH
Variously substituted 2-hydroxy-N-(arylalkyl)benzamides were prepared and screened for antiproliferative and cytotoxic activity in cancer cell lines in vitro. Five compounds, out of 33 showed single-digit micromolar IC50 values against several human cancer cell lines. One of the most potent compounds N-((R)-1-(4-chlorophenylcarbamoyl)-2-phenylethyl)-5-chloro-2-hydroxybenzamide (6k) reduced proliferation and induced apoptosis in the melanoma cell line G361 in a dose-dependent manner, as shown by decrease in 5-bromo-2'-deoxyuridine incorporation and increase in several apoptotic markers, including subdiploid population increase, activation of caspases and site-specific poly-(ADP-ribose)polymerase (PARP) cleavage.
Citace poskytuje Crossref.org
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