Abstract:
:The novel steroidal carrier ligand 17-α-[4'-ethynyl-dimethylbenzylamine]-17-β-testosterone (ET-dmba 1) and the steroid--C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA =1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC(50) were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48h incubation time complexes 2 and 3 show very low resistance factors (RF of <2) against an A2780 cell line which has acquired resistant to cisplatin and were more active than cisplatin (about 4-fold for 3) in T47D (AR+, AR=androgen receptor). Compound 1 retains a moderate degree of relative binding affinity (RBA=0.94%) for androgen receptors. The cytotoxicity of the non steroidal platinum analogues [Pt(dmba)Cl(L)] (dmba=dimethylbenzylamine; L=DMSO (4) and PTA (5)) has also been studied for comparison purposes. Theoretical calculations at the BP86/def2-TZVP level of theory on complex 3 have been undertaken.
journal_name
J Inorg Biochemjournal_title
Journal of inorganic biochemistryauthors
Ruiz J,Rodríguez V,Cutillas N,Espinosa A,Hannon MJdoi
10.1016/j.jinorgbio.2010.12.005subject
Has Abstractpub_date
2011-04-01 00:00:00pages
525-31issue
4eissn
0162-0134issn
1873-3344pii
S0162-0134(10)00286-2journal_volume
105pub_type
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abstract::The biochemically important anion, peroxynitrite, is commonly thought to have a cis-conformation which is stable. This is thought to have a cyclic structure, which blocks the formation of the trans-conformation. Furthermore, it is often suggested that the latter structure isomerises to the far more stable nitrate ion....
journal_title:Journal of inorganic biochemistry
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journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章,评审
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abstract::The putative platinum(IV) anticancer drugs, [Pt{((R)NCH(2))(2)}(py)(2)XY] (X,Y=Cl, R=p-HC(6)F(4) (1a), C(6)F(5) (1b); X,Y=OH, R=p-HC(6)F(4) (2); X=Cl, Y=OH, R=p-HC(6)F(4) (3), py = pyridine) have been prepared by oxidation of the Pt(II) anticancer drugs [Pt{((R)NCH(2))(2)}(py)(2)] (R=p-HC(6)F(4) (4a) or C(6)F(5) (4b))...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
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abstract::Two new mononuclear peroxo complexes of tungsten of the formula (gu)(2)[WO(2)(O(2))(2)] (1) and (gu)[WO(O(2))(2)(quin-2-c)] (2a) (where gu(+)=guanidinium ion, CN(3)H(6)(+) and quin-2-c=quinoline-2-carboxylate ion) have been synthesized and characterized by elemental analysis, infrared, Raman, UV-visible and (1)H NMR s...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
doi:10.1016/j.jinorgbio.2009.03.001
更新日期:2009-05-01 00:00:00
abstract::The binding of acetazolamide, p-fluorobenzensulfonamide, p-toluenesulfonamide, and sulfanilamide to nickel(II)-substituted carbonic anhydrase II has been studied by 1H NMR and electronic absorption spectroscopies. These inhibitors bind to the metal ion forming 1:1 complexes and their affinity constants were determined...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
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更新日期:1992-03-01 00:00:00
abstract::Cadmium ions applied to either (outer or inner) surface of the isolated toad skin dose-dependently increased the short-circuit current (SCC), the potential difference (V) and the active sodium conductance (G(Na)) in the concentration range 0.07-0.50mM. Maximal stimulatory effect was over 30% with an EC(50) of about 0....
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
doi:10.1016/j.jinorgbio.2005.09.003
更新日期:2005-12-01 00:00:00
abstract::Recent stopped-flow kinetics demonstrated the existence of an intermediate before the occurrence of the final product of the reaction of both iron-containing microperoxidase-8 (Fe(III)MP-8) and manganese-containing microperoxidase-8 (Mn(III)MP-8) with H(2)O(2). The intermediate was assigned to be (hydro)peroxo-iron. W...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章,评审
doi:10.1016/s0162-0134(02)00393-8
更新日期:2002-07-25 00:00:00
abstract::The purpose of the present study was to evaluate the use of a non-innocent ligand as a surrogate of the anchored [4Fe4S] cubane in a synthetic mimic of the [FeFe] hydrogenase active site. Reaction of 2,3-bis(diphenylphosphino) maleic anhydride (bma) with [Fe(2)(CO)(6)(mu-pdt)] (propanedithiolate, pdt=S(CH(2))(3)S) in ...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
doi:10.1016/j.jinorgbio.2010.05.011
更新日期:2010-10-01 00:00:00