ChemInform Abstract: Antitumor and Toxicologic Properties of the Orgnometallic Anticancer Agent Vanadocene Dichloride.

Interaction of metallocene dichlorides with apo-human transferrin: A spectroscopic study and cytotoxic activity against human cancer cell lines

“…3,4 In a clinical context,metallocene dichlorides represents the first class of small and hydrophobic organometallic compounds classified as anticancer agents with antiproliferative activity. 5,6 Several studies have established that their complexes exhibit high antitumor properties against numerous cell lines and in a wide range of murine and human tumors in vitro and in vivo 7,8 such as solid and fluid Ehrlich ascites tumors (EAT); [9][10][11][12][13][14][15] lymphoid leukemia L1210, lymphocytic leukemia P388 and L1210; 16 human breast adenocarcinoma (MCF-7); [17][18][19] human colorectal adenocarcinoma (HT-29) and Caco-2; [19][20][21][22] human testicular tumors (Tera-2 and NTera-2); 23 solid and fluid sarcoma 180; 24 solid B16 melanoma; 25 colon 38 adenocarcinoma; 25 Lewis lung carcinosarcoma; 26 mouse mammary tumor TA3Ha; 27,28 and several human colon adenocarcinomas (R85, CX-1 and C-Stg2), [29][30][31][32] human lung carcinomas (L182 and L261); 33 human breast adenocarcinoma (M3) and human stomach adenocarcinoma (M-Stg4); 34 and human renal carcinoma (KTCTL-1M, -2, -26A, -30 and -84) xenografted into athymic mice. 35 Bent metallocenes, which have a cis-dichlorometal(IV) motif similar to cis-dichloroplatinum(II) of cisplatin (CDDP) (Figure 1C), are highly efficient and effective anticancer drugs considered as one of the most promising in the treatment of different types of cancer such as testicular, ovarian, head and neck, bladder, cervical, oesophageal and small cell lung cancer.…”

Vanadocene complexes of amino acids containing secondary amino group: The first evidence of O,O-bonded carboxylic group to vanadocene(IV) moiety

“…Bis(cyclopentadienyl)vanadium(IV) complexes [Cp 2 VL 2 ] n+ (Cp = η 5 -C 5 H 5 ; L 2 -two monodentate or one bidentate ligand) have been investigated for their use in biological applications [1][2][3][4][5][6][7][8][9][10][11][12][13] since the antitumor activity of Cp 2 VCl 2 (1a) was discovered in the late seventies [14]. Recent studies show that the antitumor properties of Cp 2 VCl 2 (1a) could be improved through the substitution in the cyclopentadienyl rings.…”

Behaviour of the Antitumor Agent Vanadocene Dichloride in Physiological and Therapeutic Media, Blood Plasma and Human Blood ‐ An EPR Study

“…Its antitumor activity has been discovered by K6pf-Maier and K6pf [3]. Vanadocene dichloride was shown to be characterized by marked antiproliferative effects against some cultured animal and human tumor cells (murine Ehrlich ascites tumor [4], human KB as well as HeLa tumor [1], HEp-2 human epidermoid carcinoma [5][6][7] or normal, not transformed cells (human embryonic fibroblasts [8] ) in vitro as well as by systemic antineoplastic activity against several experimental tumor systems (fluid and solid Ehrlich ascites tumor [3,8] or TA3Ha murine mammary adenocarcinoma [5][6][7] in vivo. Various biological experiments (such as electron energy loss-spectroscopy microanalysis showing the main accumulation of vanadium in nuclear heterochromatin [9,10], precursor incorporation studies revealing inhibition of nucleic acid synthesis activities 11], cytokinetic investigations revealing mitotic depressions in tumor cells treated with I in vitro [12] and in vivo [13], cytological and morphological analysis of histological and ultrastructural alterations of animal Ehrlich ascites tumor cells treated with I in vivo [14] and human embryonic fibroblasts treated with I in vitro [8] ) pointed to the nucleic acids, especially DNA, as probable primary intracellular target for I.…”