About: Study of the anticancer properties of methyl- and phenyl-substituted carbon- and silicon-bridged ansa-titanocene complexes     Goto   Sponge   NotDistinct   Permalink

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  • The previously known complexes [Ti{(Me2CMe2C)(η5-C5H4)2}Cl2] (1), [Ti{Me2C(η5-C5H4)2}Cl2] (2), [Ti{Me2Si(η5-C5H4)2}Cl2] (4), [Ti{MePhSi(η5-C5H4)2}Cl2] (5) and [Ti{MePhSi(η5-C5Me4)2}Cl2] (6) have been prepared following reported procedures. The novel complex [Ti{MePhC(η5-C5H4)2}Cl2] (3) has been prepared and characterized. The cytotoxic activity of 1-6 has been tested after 72 h on melanoma A375 and B16, prostate cancer DU145 and LNCaP and colon cancer HCT116, SW620 and CT26CL25 cell lines observing a high cytotoxic activity of complexes 1 and 6 compared to the reference compound ([Ti(η5-C5H5)2}Cl2]). 1 and 6 have also been tested against primary normal mouse keratinocytes and lung fibroblasts. While viability of both type of primary cells was significantly less affected by 1 in comparison to the reference compound [Ti(η5-C5H5)2Cl2], compound 6 was completely nontoxic for nonmalignant cells, indicating a potential selectivity of this compound towards cancer cell lines. In addition CFSE staining, cell cycle analysis, AnnexinV-FITC/PI staining, detection of caspase activity and mitochondrial potential showed that 1 and 6 were acting through inhibition of proliferation and subsequent induction of mitochondrial dependent apoptosis in colon cancer cell lines, HCT116 and SW620, which express low sensitivity to cisplatin. Compound 6 was found to be the leading drug in this group since it shows the fastest and most selective anticancer profile.
  • The previously known complexes [Ti{(Me2CMe2C)(η5-C5H4)2}Cl2] (1), [Ti{Me2C(η5-C5H4)2}Cl2] (2), [Ti{Me2Si(η5-C5H4)2}Cl2] (4), [Ti{MePhSi(η5-C5H4)2}Cl2] (5) and [Ti{MePhSi(η5-C5Me4)2}Cl2] (6) have been prepared following reported procedures. The novel complex [Ti{MePhC(η5-C5H4)2}Cl2] (3) has been prepared and characterized. The cytotoxic activity of 1-6 has been tested after 72 h on melanoma A375 and B16, prostate cancer DU145 and LNCaP and colon cancer HCT116, SW620 and CT26CL25 cell lines observing a high cytotoxic activity of complexes 1 and 6 compared to the reference compound ([Ti(η5-C5H5)2}Cl2]). 1 and 6 have also been tested against primary normal mouse keratinocytes and lung fibroblasts. While viability of both type of primary cells was significantly less affected by 1 in comparison to the reference compound [Ti(η5-C5H5)2Cl2], compound 6 was completely nontoxic for nonmalignant cells, indicating a potential selectivity of this compound towards cancer cell lines. In addition CFSE staining, cell cycle analysis, AnnexinV-FITC/PI staining, detection of caspase activity and mitochondrial potential showed that 1 and 6 were acting through inhibition of proliferation and subsequent induction of mitochondrial dependent apoptosis in colon cancer cell lines, HCT116 and SW620, which express low sensitivity to cisplatin. Compound 6 was found to be the leading drug in this group since it shows the fastest and most selective anticancer profile. (en)
Title
  • Study of the anticancer properties of methyl- and phenyl-substituted carbon- and silicon-bridged ansa-titanocene complexes
  • Study of the anticancer properties of methyl- and phenyl-substituted carbon- and silicon-bridged ansa-titanocene complexes (en)
skos:prefLabel
  • Study of the anticancer properties of methyl- and phenyl-substituted carbon- and silicon-bridged ansa-titanocene complexes
  • Study of the anticancer properties of methyl- and phenyl-substituted carbon- and silicon-bridged ansa-titanocene complexes (en)
skos:notation
  • RIV/61388955:_____/14:00424576!RIV15-GA0-61388955
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • I, P(GAP207/12/2368)
http://linked.open...iv/cisloPeriodika
  • FEB 2014
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 48339
http://linked.open...ai/riv/idVysledku
  • RIV/61388955:_____/14:00424576
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • titanocene derivatives; cytotoxicity; primary cells (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • CH - Švýcarská konfederace
http://linked.open...ontrolniKodProRIV
  • [989EB32B9A08]
http://linked.open...i/riv/nazevZdroje
  • Journal of Organometallic Chemistry
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 751
http://linked.open...iv/tvurceVysledku
  • Pinkas, Jiří
  • Horáček, Michal
  • Bulatović, M.
  • Gómez-Ruiz, S.
  • Kaluderović, G. N.
  • Maksimović-Ivanić, D.
  • Mijatović, S.
  • Miljković, D.
  • Mojić, M.
  • Stošić-Grujičić, S.
http://linked.open...ain/vavai/riv/wos
  • 000329864700031
issn
  • 0022-328X
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.jorganchem.2013.07.059
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