Synthesis and biological evaluation of structurally related colchicine compounds as potential anticancer agents /
تشييد و تقييم بيولوجى لمركبات ذات علاقة بتركيب الكولشيسين كمضادات محتملة للسرطان
Amira Youssef Adib Youssef ; Supervised Salwa M. Elmeligie , Azza T. Taher Shalaby , Aliaa M. Kamal
- Cairo : Amira Youssef Adib Youssef , 2017
- 94 P. ; 25cm
Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry
This thesis comprises four chapters. The first one is an introduction which consists of a brief survey on the chemistry and biological activity of structurally related colchicine compounds and their cytotoxic activity. The second chapter deals with the aim of the work based on structure activity relationship along side the schemes that have been carried out to obtain the structurally related colchicine compounds. The third chapter presents the theoretical discussion of the experimental work in the preparation of chalcone derivatives Ia-i which were prepared from the appropriate substituted acetophenone and substituted benzaldehyde via claisen-schmidt condensation reaction. Cyclization of Ia, Ib, Ie, If, Ig, Ih and Ii with thiourea gave 4-(4-substitutedphenyl)-6-( substitutedphenyl)-3,4-dihydropryimidine-2(1H)-thione (IIa-g). Cyclization of Ia, Ib, Ic and Id with hydrogen peroxide in the presence of sodium hydroxide solution gave 3-(4-substitutedphenyl) oxirane-2-yl) (substitutedphenyl)methanon(IIIa-d).5-(4-substitutedphenyl)-3-(substitutedphenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-4-ol (IVa-d) were synthesized via the reaction of compounds IIIa-d with phenylhydrazine and 5-(4-substitutedphenyl)-3-(3-methoxyphenyl)-4, 5-dihydro-1H-pyrazol-4-ol (IVe and IVf) prepared via the reaction of compounds IIIa and IIIb with hydrazine hydrate