The molecular structure of trimethylantimony(V) dichloride has been studied in the gas phase at 150°C. The chlorine atoms are found to be in the axial position of the trigonal bipyramid. The geometrical parameter values obtained from least-squares analysis are: r(CH) = 1.10(1) Å, r(SbC) = 2...

The infrared and Raman spectra of trimethylantimony oxide and its deuterated analogue were recorded. Assignments were made and a normal coordinate analysis was carried out. A polar coordinate linkage is proposed for the SbO bond.

In our study, we demonstrate that trimethylantimony dichloride (TMSb) does not induce micronucleus (MN) formation, chromosome aberrations (CA) or sister chromatid exchanges (SCE) under normal conditions in Chinese hamster ovary (CHO-9) cells in vitro up to an applied concentration of 1 mM, nor i...

Trimethylantimony was detected with high frequency in the headspace of Scopulariopsis brevicaulis cultures during aerobic growth. The compound was formed biologically from potassium antimony tartrate and no other volatile antimony species were detected. Complete biomethylation of antimony (III) ...

The objective of this study was to determine the elimination kinetics of extended therapy with intramammary (IMM) cephapirin in lactating dairy cattle. Eight healthy Holstein-Friesian cows were administered cephapirin (200 mg) into all 4 mammary glands every 24 h after milking. Cows were milked ...

A specific, stability-indicating, high-performance liquid chromatographic assay was developed for the determination of cephapirin, desacetyl cephapirin and cephapirin lactone in sodium cephapirin (cafedyl) bulk and injectables. The procedure uses a μBondapak C18 column and a mobile phase of dim...

Thymidine phosphorylase (TP) is an enzyme that promotes tumor growth and metastasis and therefore is an attractive druggable target. Using a reported TP inhibitor, 7-deazaxanthine (7DX), as the lead compound; this study was set up to evaluate whether pyrazolo[1,5-a][1,3,5]triazin-2,4-diones and ...

3-Formylchromone (1), 3-methyl-7-hydroxychromone (2) and Schiff bases of 3-formylchromone 3–19 have been synthesized and their anti-thymidine phosphorylase inhibitory activity was evaluated. Compounds 1–19 showed a varying degree of thymidine phosphorylase inhibition with IC50 values 19.77 ± ...

The dinuclear Ni2+ and Zn2+ complexes of 1,1′-[(1H-pyrazole-3,5-diyl)bismethylene]-bis(octahydro-1H-1,4,7-triazonine) induce phosphate diester hydrolysis in biological relevant substrates such as thymidine 5′-monophosphate 4-nitrophenylester (TMPNP), guanosine (2′-3′) cyclic phosphate ((2′-...

Thymidine phosphorylase (TP) inhibitors have attracted great attention due to their ability to suppress the tumors formation. In our ongoing research, a series of 1,3,4-oxadiazole-2-thione (1–12) has been synthesized under simple reaction conditions in good to excellent yields (86–98%) and the...

A series of novel 1,3,4-oxadiazole-2-thione derivatives were designed, synthesized and evaluated for in vitro anticancer activity against breast cancer (MCF-7) cell line and thymidine phosphorylase. The synthesis of target compounds was performed by cyclization reaction using aromatic amines and...

The separated diastereomers of 3′-(4-nitrophenyl N-phenyl phosphoramidate)-5′-monomethoxytrityl thymidine and 3′-monomethoxytrityl-5′-(4-nitrophenyl N-phenyl phosphoramidate) thymidine have been prepared and their absolute configurations at phosphorus have been determined.

Inhibition of Thymidine phosphorylase (TP) is continuously studied for the design and development of new drugs for the treatment of neoplastic diseases. As a part of our effort to identify TP inhibitors, we performed a structure-based virtual screening (SBVS) of our compound collection. Based on...

Thymidine phosphorylase triggers the phosphorylation of pyrimidine base to thymine and 2-deoxyribose 1-phosphate which undergoes dephosphorylation to 2-deoxyribose. It plays a role in tumor angiogenesis which is referred to the development of blood vessels during tumor growth and therefore is an...

Thymidine phosphorylase (TP) is over expressed in several solid tumors and its inhibition can offer unique target suitable for drug discovery in cancer. A series of 1,2,4-triazoles 3a–3l has been synthesized in good yields and subsequently inhibitory potential of synthesized triazoles 3a–3l ag...

Isoquinoline analogues (KA-1 to 16) have been synthesized and evaluated for their E. coli thymidine phosphorylase inhibitory activity. Except compound 11, all other analogs showed outstanding thymidine inhibitory potential ranging in between 4.40 ± 0.20 to 69.30 ± 1.80 µM when compared with s...

The pure rotational spectrum of a Claisen rearrangement precursor, Allyl Phenyl Ether (APE), has been measured on a chirped pulse Fourier transform microwave (CP-FTMW) spectrometer in the 8–14 GHz region. Rotational and centrifugal distortion constants for multiple conformations have been deter...

The crystal structure of the salt produced by the reaction of pyrimethamine (an antimalarial drug) with 2-hydroxy-3,5-dinitrobenzoic acid [systematic name: 2,4-diamino-5-(4-chlorophenyl)-6-ethylpyrimidin-1-ium 2-hydroxy-3,5-dinitrobenzoate] has been investigated using X-rays diffraction data col...

6-Hydroxytropanone (8) was synthesized by a Mannich type condensation between acetonedicarboxylic acid, methylamine hydrochloride, and the hydrolysis product of 2,5-dimethoxydihydrofuran and was used as the key intermediate for the synthesis of the four racemic isomers of 6β-hydroxy-2-(methoxyc...

A chemoselective domino annulation reaction of β-naphthols with methyl aryldiazoacetate is described. The gold catalyst promoted C–H functionalization of β-naphthols, whereas a rhodium or copper complex led to O–H insertion reactions. Consecutive intramolecular lactonization occurred after s...