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Anti tumor activity of metallocenes substituted or bridged titanocene di chlorides



Anti tumor activity of metallocenes substituted or bridged titanocene di chlorides



European Journal of Medicinal Chemistry 16(3): 275-281



Monosubstituted, 1,1'-disubstituted and 1,1'-bridged titanocene dichlorides (RC5H4)(C5H5)TiCl2 (R = Me, Et, SiMe3; 1-3), (RC5H4)2 TiCl2 (R = Me, CMe3, SiMe3, SiMe2Bu, GeMe3; 4-8) and Z(C5H4)2TiCl2 (Z = (CH2)3, CH2, CHMe, SiHMe, SiEt2, GeMe2; 9-15) were prepared by metallation of cyclopentadienes RC5H5 and Z(C5H5)2 with BuLi and by the following reaction with C5H5TiCl3 or TiCl4, respectively. The resulting compounds 1-15 and the indenyl and tetrahydroindenyl derivatives (C9H7)2TiCl2, (C9H11)2 TiCl2 and (C9H11)(C5H5)TiCl2 (16-18) were investigated with regard to their antitumor activity against [mouse] Ehrlich ascites tumor cells and mice. Complexes 2, 3 and 18 which are modified only at 1 cyclopentadienyl ring, show optimum cure rates of 80, 60 and 100%. These values are only slightly diminished in comparison to the unsubstituted titanocene dichloride; the tumor-inhibiting activity of complexes containing 2 modified C5H5 rings (4-17) is strongly reduced. The weakening influence of chemical variation at the cyclopentadienyl rings on the tumor-inhibiting activity of metallocene dihalides is in agreement with the hypothesis of a carrier function of these 5-membered ring ligands.

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