The potent and selective Cyclin-Dependent Kinase 2 (CDK2) inhibitor NU6027 (6-cyclohexylmethoxy-5nitroso-2,4-diaminopyrimidine) was used as the lead for the synthesis of a series of analogues in order to provide further insights into the structure activity relationships for 2,4-diaminopyrimidine CDK2 inhibitors. Aliphatic amino substituents were introduced at position 2. The use of linear or le...

A new viscometric technique, capable of detecting DNA strand breaks and alkali-labile sites by monitoring time-dependent changes of DNA-reduced viscosity, has been used to analyze dose-response curves for the induction of DNA damage in liver of rats treated with single p.o. doses of sixteen N-nitroso compounds. Statistically significant changes of DNA viscometric parameters, which are considere...

In the title compound, C(14)H(9)NO(2), a static disorder exists between the keto-oxime and hy-droxy-nitroso tautomers, in an approximate ratio of 4.6:1, based on refined occupancies for disordered parts. No inter-molecular hydrogen bonding is present in the crystal structure. Instead, both tautomers exhibit similar intra-molecular O-H⋯O hydrogen bonds.

A series of fluoroquinolone compounds (compounds 1-9), which contain a common quinolone scaffold, inactivated the metabolic activity of CYP3A. The purpose of this study was to identify mechanism-based inhibition (MBI) among these fluoroquinolone compounds by metabolite profiling to elucidate the association of the substructure and MBI potential. Reversibility of MBI after incubation with potass...

In the centrosymmetric title compound, [Cu(C5H11N2O2)2], the Cu(2+) ion, located on an inversion centre (Wyckoff position 2b), is in a square-planar environment, surounded by four O atoms of the N-O groups of two N-nitroso-N-pentyl-hydroxy-laminate ligands [Cu-O = 1.9042 (17) and 1.9095 (16) Å]. The hy-droxy-laminate monoanions are bidentate chelating ligands. The Cu(2+) cations form stacks alo...

The four cupferronate ions in the dinuclear title compound, [Pb(2)(C(6)H(5)N(2)O(2))(4)], O,O'-chelate to the two Pb(II) atoms; two of the four nitroso O atoms are also involved in bridging. The geometry of both five-coordinate Pb(II)atoms is distorted Ψ-octa-hedral; if another two longer inter-molecular Pb⋯O inter-actions [at 2.955 (1) and 3.099 (1) Å] are considered, the geometry is a distort...

(1) Background: The aim of this study was to identify the degradation product ramipril (RAM) formed under dry air and verify its potential modes carcinogenicity. We intended check whether formation presence in final dosage forms could pose a cancer risk humans who are treated with RAM due cardiological indications. carcinogenicity compound evaluated respect two mechanisms: direct DNA-damage ind...