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Abstract
In this thesis, novel series of colchicine binding site inhibitors (CBSIs) were designed. Molecular modeling techniques were used to support the design. Chalcones derivatives IIa - d, cyclohexenone derivatives IIIa,b, IVa,b, cyanopyridine derivatives VIa, b, isoxazoline derivatives VIIa - d, pyrazoline derivatives VIIIa, b, IXa, b, Xa - f, XIa, b and XIIa - f were synthesized. Eight target compounds were evaluated for antitumor activity at National cancer institute, NCI, maryland, USA against several cell lines. Twenty four target compounds were evaluated for antitumor activity and their ability to inhibit tubulin polymerization against leukemia SR cell line at Vacsera, Egypt