Design, synthesis and anti-tumour activity of new pyrimidine-pyrrole appended triazoles.

The new pyrimidine-pyrrole scaffolds (7a-7m) with substituted 1,2,3-traizole moiety were synthesized in good to mild yields and subjected for anti-cancer activity against melanoma and breast cancer cell lines using MTT assay. The compounds 7f and 7m exhibited highest anti-cancer activity against both the tested cell lines in in vitro assay. The molecular docking analysis provided the insights of binding orientation of pyrimidine-pyrrole nucleus of current ligands and their crucial interactions with Cys797 and other residues of the EGFR tyrosine kinase active site.

Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives.

Novel N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives were designed, synthesized and their chemical structures were confirmed by H NMR, C NMR and Mass spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including K562, Colo-205 and MDA-MB 231 by MTT assay. The screening results showed that five compounds (16b, 16d, 16i, 16p and 16q) exhibited potent cytotoxic activities with IC values between 20 and 40μM.

Determination of genotoxic impurity in atazanavir sulphate drug substance by LC-MS.

A sensitive LC-MS method was developed for the determination of tert-butyl 2-[4-(pyridine-2-yl) benzyl] hydrazine carboxylate (GTI-A), a genotoxic impurity in Atazanavir sulphate drug substance. The method was validated as per International Council for Harmonization guidelines, for QL, DL, linearity and accuracy. The QL and DL values obtained were 1.