Chalcones (1,3-diaryl-2-propen-1-ones) are a, b-unsaturated ketones with cytotoxic and anticancer properties. Several reports have shown that compounds with cytotoxic properties may also interfere with DNA topoisomerase functions. Five derivatives of 4 0 -hydroxychalcones were examined for cytotoxicity against transformed human T (Jurkat) cells as well as plasmid supercoil relaxation experiments using mammalian DNA topoisomerase I. The compounds were 3-phenyl-1-(4, and 3-(2-thienyl)-1-(4 0 -hydroxyphenyl)-2-propen-1-one (V). The order of the cytotoxicity of the compounds was; IV > III > II > I > V. Compound IV, had the highest Hammett and log P values (0.23 and 4.21, respectively) and exerted both highest cytotoxicity and strongest DNA topoisomerase I inhibition. Compounds I and II gave moderate interference with the DNA topoisomerase I while III & V did not interfere with the enzyme.

A group of N-phenylacetamide derivatives bearing five membered heterocyclic rings, pyrazole or 1,2,4-triazole, were synthesized to investigate their cholinesterase inhibitory activities. Acetylcholinesterase (Ache) and butyrylcholinesterase (Buche) inhibitory activities were evaluated by using ellman's spectroscopic method. results indicated that all of the compounds displayed moderate and selective Ache inhibitory activity and the most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(3-methoxyphenyl)acetamide with an ıc 50 value of 6.68 mM. Docking studies were also carried out for the most active compound.

In this study, 15 compounds bearing N,N-phthaloylacetamide structure designed by the molecular simplification approach based on thalidomide structure were synthesized and evaluated for inhibitory potencies against cyclooxgenase (COX) isoenzymes, namely COX-1 and COX-2. The results suggested that the N,N-phthaloylacetamide structure, as a primary amide, has inhibitory activity against cyclooxygenase isoenzymes with a higher COX-1 selectivity. The conversion of the primary amide to secondary or tertiary derivatives lowered the potency but favored the COX-2 selectivity thus yielding the compounds with stronger COX-2 inhibiting activity.

. -New isoindoline derivatives (II), (IV), and (VI) are evaluated for their inhibitory potencies against cyclooxogenases (COX-1 and COX-2). Primary amides show inhibitory activities against isoenzymes with a higher COX-1 selectivity, whereas secondary as well as tertiary amides show stronger COX-2 inhibiting activities. -(CIZMECIOGLU, M.; PABUCCUOGLU, V.; BALLAR, P.; PABUCCUOGLU, A.; SOYER*, Z.; Arzneim. -Forsch. 61 (2011) 3, 186-190

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