The biliary excretion and blood/plasma ratios of four novel 5-bromo-6-alkoxy- 5,6-dihydro prodrugs to S-ethyl-2'-deoxyuridine (EDU) including (-)-trans-(5S, 6S)-S-bromo-S-ethyl-6-methoxy-S, 6-dihydro-2'-deoxyuridine (BMEDU), (+ )-trans( SR, 6R)-S-bromo-S-ethyl-6-ethoxy-S, 6-deoxyuridine (BEEDU), (+ )-trans-(SR, 6R)-5-bromo-5-ethyl-6-ethoxy -S, 6-dihydro-S '-O-valeryl-2 ':.deoxyuridine (VBE...

Introduction: Fluoroquinolones are potent inhibitors of bacterial topoisomerase II. They can also inhibit eukaryotic topoisomerase, and may confer antitumoral properties. Method: In this study the antitumoral activity of a new series of N-substituted piperazinylfluoroquinolones against a panel of human tumor cell lines was determined by MTT assays. Results: Among the tested compounds N-[2- (5-b...

A new derivative of zirconium (IV), [(acac)2Zr{ONC(Me)th-2}2] have been produced by treating bis(acetylacetonato)diisopropoxy zirconium(IV) with internally functionalised oxime HONC(Me)th-2 (where th = thiophene) in 1:2 stoichiometry, while refluxing in anhydrous toluene. After drying and purification, the product appeared as offwhite crystalline solid. Physico-chemical analysis of this derivat...

Biscyclometalated iridium(III) complexes with an ancillary acetylacetone ligand, Ir(L)(2)(acac), (L = 2-(benzo[b]thiophen-2-yl)pyridine (btp), 1-phenylisoquinoline (piq), 2-phenylbenzothiazole (bt), 2-phenylpyridine (ppy), acac = deprotonated acetylacetone), demonstrate spectroscopic changes in their UV-Vis absorption and luminescent emission under acidic conditions. Such changes were found to ...

Abstract Coumarin and its nitrogen analogue 1-aza coumarin are a class of lactones lactams, respectively, which indispensable heterocyclic units to both chemists biochemists. 1-Aza derivatives, ultimately metabolize as the corresponding 8-hydroxy coumarins in biological system therefore found be very good anti-inflammatory, anti-cancer, analgesic agents. A series hybrid substituted azacoumarin-...

synthesis of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-[4-(2-substitutedphenyl-4-oxo-thiazolidinyl)aryl]-6-bromo quinazolin-4(3h)ones via-j have been achieved from the starting material 2-[(2,6-dichlorophenyl)amino] phenylacetic acid i to benzoxazine iii, further reaction with p-phenylindiamine and substituted aromatic aldehyde gave 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-(4-aminoary...

Esterification of p-bromo-m-cresol led to formation of 2-(4-bromo-3-methylphenoxy)acetate (1). 2-(4-Bromo-3-methyl phenoxy)acetohydrazide (2) is derived from Compound (1) by hydrazination. Compound (2) was reacted with different aromatic aldehydes to yield N-(substituted benzylidiene)-2-(4-bromo-3-methyl phenoxy)acetamide(3a-c). Cyclization of compound (3a-c) with thioglycolic acid yielded 2-(4...