تفاصيل الرسالة العلمية

The work presents the synthesis of new series of 6-(chlorothiophenyl)-2-(2-oxopropoxy)pyridine-3-carbonitrile compounds and their furo[2,3-b]pyridines bearing hetero aryl substituents in high yield. The 6-(chlorothiophenyl)-2-(2-oxoprop-oxy)pyridine-3-carbonitrile derivatives (62a-f) and (63a-d) were prepared from the corresponding 3-cyano-(2H)-pyridones (60a-f) and (61a-d) followed by the Thorpe-Ziegler ring cyclization in the presence of sodium methoxide to give the target furo[2,3-b]pyridine derivatives (64a-f) and (65a-d).The structure of all new compounds were proposed based on the NMR and mass spectrometry spectral data. Compounds (62a), (62c-e), (63a-b), (63d), (64a), (64c-e), (65a-b) and (65d) were subjected for the antibacterial activity against eight different microorganisms and for cytotoxic activity against MCF7 breast cancer cell. None of the derivatives was active towards any of the tested bacteria with compounds )65a( and )65e( only showed weak antibacterial activity with inhibition zone of 10 mm. Cytotoxic activity assessment reveals that 10 of the derivatives were found to decrease cell viability in a dose dependent manner at concentration of 100?M, but Six of them decreased it to less than 50% and had IC50?s ranging from 23.3 to 41.2 ?M.