Literature DB >> 16764931

Heteroaryl substituted titanocenes as potential anti-cancer drugs.

Nigel Sweeney1, William M Gallagher, Helge Müller-Bunz, Clara Pampillón, Katja Strohfeldt, Matthias Tacke.   

Abstract

From the reaction of Super Hydride (LiBEt(3)H) with 6-(furyl)fulvene (1a), 6-(thiophenyl)fulvene (1b) or 6-(N-methyl-pyrrole)fulvene (1c) the corresponding lithium cyclopentadienide intermediates (2a-c) were obtained. These intermediates were reacted with titanium tetrachloride and bis-[(furyl-2-cyclopentadienylmethane)] titanium(IV) dichloride (3a) and bis-[(thiophenyl-2-cyclopentadienylmethane)] titanium(IV) dichloride (3b) and bis-[(N-methylpyrrole-2-cyclopentadienylmethane)] titanium(IV) dichloride (3c) were obtained and subsequently characterised by X-ray crystallography. When titanocenes 3a-c were tested against pig kidney (LLC-PK) cells inhibitory concentrations (IC(50)) of 1.6x10(-4)M, 1.5x10(-4)M and 9.1x10(-4)M, respectively, were observed. These values represent improved cytotoxicity against LLC-PK, when compared to their corresponding ansa substituted analogues and also in comparison to unsubstituted titanocene dichloride.

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Year:  2006        PMID： 16764931     DOI： 10.1016/j.jinorgbio.2006.04.006

Source DB:  PubMed          Journal:  J Inorg Biochem        ISSN： 0162-0134            Impact factor:   4.155


  7 in total

1.  Synthesis and cytotoxicity studies of steroid-functionalized titanocenes as potential anticancer drugs: sex steroids as potential vectors for titanocenes.

Authors:  Li Ming Gao; José L Vera; Jaime Matta; Enrique Meléndez
Journal:  J Biol Inorg Chem       Date:  2010-03-28       Impact factor: 3.358

2.  Titanium(IV) complexes: cytotoxicity and cellular uptake of titanium(IV) complexes on caco-2 cell line.

Authors:  Ramón Hernández; Janet Méndez; José Lamboy; Madeline Torres; Féliz R Román; Enrique Meléndez
Journal:  Toxicol In Vitro       Date:  2009-09-20       Impact factor: 3.500

3.  Water-soluble molybdenocene complexes with both proliferative and antiproliferative effects on cancer cell lines and their binding interactions with human serum albumin.

Authors:  Idainés Feliciano; Jaime Matta; Enrique Meléndez
Journal:  J Biol Inorg Chem       Date:  2009-06-18       Impact factor: 3.358

4.  Dimethylamino-functionalised and N-heteroaryl-substituted titanocene anticancer drugs: synthesis and cytotoxicity studies.

Authors:  Thomas Hickey; James Claffey; Eoin Fitzpatrick; Megan Hogan; Clara Pampillón; Matthias Tacke
Journal:  Invest New Drugs       Date:  2007-05-22       Impact factor: 3.850

5.  Synthesis and Antitumor Activity of New Group 3 Metallocene Complexes.

Authors:  Angelamaria Caporale; Giuseppe Palma; Annaluisa Mariconda; Vitale Del Vecchio; Domenico Iacopetta; Ortensia Ilaria Parisi; Maria Stefania Sinicropi; Francesco Puoci; Claudio Arra; Pasquale Longo; Carmela Saturnino
Journal:  Molecules       Date:  2017-03-28       Impact factor: 4.411

6.  Synthesis and cytotoxicity studies of titanocene C analogues.

Authors:  Megan Hogan; James Claffey; Eoin Fitzpatrick; Thomas Hickey; Clara Pampillón; Matthias Tacke
Journal:  Met Based Drugs       Date:  2008

7.  Substituted titanocenes induce caspase-dependent apoptosis in human epidermoid carcinoma cells in vitro and exhibit antitumour activity in vivo.

Authors:  J H Bannon; I Fichtner; A O'Neill; C Pampillón; N J Sweeney; K Strohfeldt; R W Watson; M Tacke; M M Mc Gee
Journal:  Br J Cancer       Date:  2007-10-09       Impact factor: 7.640
  7 in total

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