Novel tetrahydronaphthyl thiazole derivatives of anticipated anticancer activity

A new series of some new N-arylidene-4-[1,2,3,4-tetrahydr onaphthalene-6-yl]thiazol-2-amine Schiff bases Il cyclized either by thioglycolic acid or thiosalicylic acid afforded thiazolidinone and benzothiazine derivatives III and IV, respectively. Also, amine I condensed with alpha-halocarbonyl compounds to give the corresponding amino derivatives V. Cyclocondcnsation of the chloroacetamido derivative Vd gave the pyrazine, quinoxaline, benzoxazine and chlorobenzoxazine derivatives VI-VIIIb, respectively. Compounds IIc, III, Vb, VI are evaluated as anticancer agents in human liver carcinoma cell line [HePG2] and breast carcinoma cell line [MCF7] and showed promising activities against these two cell lines

Changes in vaginal microflora and bone resorbing cytokines level in postmenopausal period

This study was designed to evaluate the role of postmenopausal estrogen deficiency on vaginal microflora, detect its relation with level of bone resorbing cytokines and to evaluate their role in postmenopausal osteoporosis. One hundred and twenty females were investigated. They were divided into two groups, Group I included 60 women in postmenopausal period, Group II [control group] included 60 women in premenopausal period. All of them were subjected to bacteriological examination: vaginal swabs were used for making direct Gram-stained smears but only 100 specimens [50 from each group] were cultured on suitable culture media to isolate different vaginal microorganisms and compare the isolates of the two tested groups. Eighty females [40 from each group] were subjected to serological studies including estimation of serum level of interleukin-6, interleukin- 1 beta, and tumor necrosis factor-alpha] using enzyme immunoassay [EIA] technique, estradiol and osteocalcin levels were measured by radioimmunoassay [RIA] technique. The study revealed that vaginal flora in postmenopausal females, according to Nugent Scoring System, showed normal pattern [82%] Intermediate [15%] and bacterial vaginosis [3%] compared with 72%, 23% and 5% respectively in premenopausal females with no statistically significant difference between the two groups [P>0.05]. There was a lower isolation rate of facultative Lactobacilli, Gardnerella vaginalis, C and ida albicans and Mobiluncus in postmenopausal females than in premenopausal females. Catalase +ve Lactobacilli was found to be predominant over catalase -ve in both post- and premenopausal females although their rate of isolation was lower in premenopausal females. In most of the cases, which showed bacterial vaginosis, G. vaginalis were isolated in high percentage associated with catalase-ve Lactobacilli. There was higher level of estradiol in sera of premenopausal than in postmenopausal females with statistically significant difference between them [P<0.001]. Serum level of osteocalcin was elevated in post- than in premenopausal females with no statistically significant difference between them [P>0.05]. There was also no statistically significant correlation between osteocalcin and age, parity, body mass index and estradiol level. A higher serum level of IL-6 and TNF-alpha was found in post- than in premenopausal females with statistically significant difference between them [P 0.05]. These factors showed no statistically significant correlation with serum level of both estradiol and osteocalcin [P>0.05]. Estrogen replacement therapy is recommended for postmenopausal females with more attention must be paid to personal hygienic measures for protection against colonization of vagina with potentially pathogenic microorganisms. Moreover, detection of bone resorbing cytokines level in bone microenvironment together with their estimation in serum are more important tool to evaluate the role of postmenopausal estrogen deficiency on bone resorption

Synthesis and reactions of 2- [2, [2, 4, 6-trimethyl benzoyl] Vinyl] -4H-3, 1-benzoxazin-4-one of expected biological activity

Beta-[2,4,6-trimethyibenzoyl]- acryloyl chloride reacts with anthranilic acid to give [1] which is easily cyclized by the action of acetic anhydride to give the Benzoxazone[2]. Condensation of [2] with hydrazine hydrate give [3]. The behaviour of [3] towards the action of aromatic aldehydes, ketones, phthalic anhydride and phthalyl amino acid chlorides has been investigated. Reactions of [2] with o-phenylene diamine, ammonia, grignard reagents, friedl-crafts reaction and bomine has been described

reaction of hydrazines with B-aroyl acrylic acids and their methyl esters

It has been reported that Beta-benzoylacrylic acid and its methyl ester react with hydrazines to give variable products according to the experimental conditions

Michael condensation of B- [2tetroyl] -acrylic acid and hetero-ring formation via reaction of 3- [2-tetralyl] -6-acetyl-5-oxo-3-cyclohexene-1carboxylic acid with some nucleophelic reagents

In continuation to our recent study Beta-[2-tetroyl]-Acrylic acid [I] reacts under Michael conditions with acetylacetone to give 3-[2-tetralyl]-6-acetyl-5-oxo-3-cyclohexene-l- carboxylic acid [II]

Synthesis and some reactions of -phenyl-B-9-anthroylpropionic acid

Reaction of Beta-9-anthroylacrylic acid [I] with benzene under Fried el-Crafts conditions gave the corresponding alpha-phenyl-Beta-9-anthroyl propionic acid [II]. Dehydration of II with Ac2O gave the butenolide III which reacts with amines to give anilides. IV. Condensation of II with hydrazines gave the corresponding hydrazones V and pyridazinone derivatives VI, and with hydroxyl-amine hydrochloride to give oxime VIII and dihydroxazinone derivative IX. Estrification of II using methanol and dry HC1 gave the methyl ester X. Reaction of X with hydrazines has been investigated

Synthesis and some reactions of new 3, 1 nbenzosazine-4- one derivatives

2[2,5-Dimethylbenzoyl vinyl]-4H -3, j-benzoxazin-4 -one [II] can be obtained via reaction of B-[2,5-dimethylbenzoyl]-acrylyl chloride with anthranilic acid followed by cyclization of the anilide [I] formed by the action of Ac2O. The action of amines, hydrazines, hydroxylamine hydrochloride, urea and thioureas on the benzoxazone has been investigated

Synthesis of some new 2- [2 [chlorobenzoyl] vinyl] -4H-3, 1-quinazolin-4-one derivatives

Several 2-[2-[p-chlorobenzoyl] vinyl] -4H-3, l-quinazolin-4-one derivatives have been synthesized by the reaction of 2-[2-p-chlo-robenzoyl] vinyl]-4H-3,l-benzoxazin-4-one with amino compounds. The action of hydrazines, hydroxylamine hydrochloride, urea, thiourea, and P2S5 have been also investigated

Synthesis of some new benzoxazone and quinazolone derivatives

2-[2-aroylvinyl-4H-3,l-benzoxazin-4-one [IIa and b] were obtained via shaking an ether solution of anthranilic acid with Beta-aroylacrylyl chlorides followed by cyclization using Ac2O. The reaction of [IIa and b] with amines, hydrazines, hydroxylamine hydrochloride, urea and thiourea has been investigated