Potential Antitumour Agent Research Articles

Antitumour activity of chlorimidazine on transplantable mouse tumour systems.

The antitumour activity of the newly synthesized compound, chlorimidazine (1-chlorethyl-2-chlormethyl-2-imidazoline hydrochloride), has been investigated on mouse tumour systems including L 1210 and P 388 leukaemias and Lewis lung carcinoma. It has been found that optimum treatment schedules resulted in 153% T/C in mice with L 1210 leukaemia, 159% T/C in mice bearing P 388 leukaemia and 68% TWI for Lewis lung carcinoma. Due to the results obtained the compound acts as a novel potential antitumour agent that warrants further evaluation.

1-Naphthol: A potential selective antitumour agent

1-Naphthol: A potential selective antitumour agent

Metal complexes of pyrimidine-derived ligands—III: Tris-complexes of Co(III), Ni(II) and Cu(II) fluoroborates, perchlorates and iodides with 3,5-dimethyl-1-(4′,6′-dimethyl-2′-pyrimidyl) pyrazole, a potential anti-tumour agent

Tris-complex of Co(II), Ni(II), Cu(II) fluoroborates, perchlorates and iodides with the title ligand conform to the composition M(DPymPz) 3X 2, nH 2O [M = Co(II), Ni(II), Cu(II); X = ClO 4, BF 4 and I, n = 0,2]. Physico-chemical characterisations of the complex species have been made from electronic and vibrational spectra, magnetic susceptibility measurements in the solid state and conductivity measurements in solution. Electronic spectral features together with the corresponding ligand field parameters suggest an overall octahedral environment for the pyrazolyl nitrogen (tertiary) and one of the pyrimidyl nitrogens as bonding sites in forming these complexes while the anion (X) retains its identity (as in free form) in the said species.

Highly fluorinated analogues of pharmacologically active compounds.

The pentafluorophenyl analogues of noradrenaline, adrenaline, and N-methyladrenaline [C6F5·CH(OH)·CH2·NR1R2 with R1= R2= H; R1= H, R2= Me; R1= R2= Me, respectively] have been prepared by reduction with sodium borohydride of the corresponding amino-ketones obtained by standard methods. 3-(N-2-Chloroethyl-N-ethyl)-aminomethyl-4,5,6,7-tetrafluorobenzo[b]thiophen has also been synthesised as a potential catecholamine antagonist and anti-tumour agent, by a method involving the cyclisation with polyphosphoric acid of 2,3,4,5-tetra-fluorophenylthiopropanone to give the expected 4,5,6,7-tetrafluoro-3-methylbenzo[b]thiophen, and thence by standard methods. The above pentafluorophenyl compounds are only very weak catecholamine antagonists.

Hydrolysis of di(aziridin-1-yl)sulphoxide to ethyleneimine.

DI(AZIRIDIN-l-YL)SULPHOXIDE (DESO), which was synthesized as a potential anti-tumour agent, has been shown to possess the property of liberating ethyleneimine in the presence of phosphate ion1. This communication reports a more detailed investigation of this effect. Ethyleneimine assay involved the colorimetric measurement (at 420 mµ) of the chloroform extract able dye obtained by reaction of the base with 1,2-naphthaquinone-4-sodium sulphonate in barbitone buffer (0.1 M, pH 9.6). The production of ethyleneimine from DESO was verified by comparing the absorption curves of the dyes derived from ethyleneimine and DESO (absorption maxima 303 and 425 mµ). On incubating DESO (2 mg/ml., 37° C) for 2 h in barbitone buffer over the pH. range 6.4–8.0 there was never more than 3 per cent hydrolysis, but at pH. 6.5 in phosphate buffer there was 74 per cent conversion to ethyleneimine. DESO was also quite stable on incubation in water, but addition of phosphate buffer resulted in the rapid production of ethyleneimine1.