SYNTHESIS AND ANTICANCER SCREENING OF HETEROCYCLIC COMPOUNDS BEARING PYRIMIDO [4, 5-B] QUINOLINE MOIETYAbstract
Due to your efforts diligent on quinoline nucleus new series containing pyrimido [4, 5-b] quinoline were synthesized via starting with the strategic 2-aminoquinoline-3-carbonitrile (2) intermediates to afford various pyrimido [4, 5-b] quinoline via cyclization with different reagents to get compounds 3-24. Compounds 3, 6, 9a, 9b, 12, 15, 16a, 16b, 17, 21 and 24 were tested for in vitro antitumor activity against human breast carcinoma (MCF-7) cell line, We found what we were hoping for where compound 6 was found the most active member (IC50= 48.54 μM) than the Doxorubicin as a reference drug with (IC50= 71.80 μM). To understand the interaction of binding sites with the target protein receptor, the docking study was performed using topoisomerase II. The results of in vitro cancer activity and docking study revealed that the synthesized compounds have potential cancer activity and can be further optimized and developed as a lead compound.
Kamal M. El-Gamal
Organic Chemistry Department, Al-Azher University (Boy’s) , Nasser City, Cairo, Egypt
03 August, 2016
03 October, 2016
06 December, 2016
01 February, 2017