Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.
In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid chloride derivative(4), followed by conversion into the corresponding acid hydrazide derivative (5) carboxylic acid thiosemicarbazide (11), esters
... Show MoreThis research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4- tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2)
... Show MoreShumblan (SH) is one of the most undesirable aquatic plants widespread in the irrigation channels and water bodies. This work focuses on boosting the biogas potential of shumblan by co-digesting it with other types of wastes without employing any chemical or thermal pretreatments as done in previous studies. A maximum biogas recovery of 378 ml/g VS was reached using shumblan with cow manure as inoculum in a ratio of 1:1. The methane content of the biogas was 55%. Based on volatile solid (VS) and C/N ratios, biogas productions of 518, 434, and 580 ml/g VS were obtained when the shumblan was co-digested with food wastes (SH:F), paper wastes (SH:P), and green wastes (SH:G) respectively. No significant changes of methane contents were observ
... Show MoreKE Sharquie, RA Najim, RK Al-Hayani, AA Al-Nuaimy, DM Maroof, Saudi medical journal, 2008 - Cited by 74
I've been in this research preparation and diagnostic complexes mixed Kandat of Alcavaúan Alpiculan ion Althaaossianat with some metal ions has been reactive in ethanol solvent and distilled water by (1:1) and water complexes and lotions to the accounts of the metal in the complex
Background: A successful endodontic treatment is aimed at the sterilization of the entire pulp space. The use of extracts from Rhamnus prinoides as a novel irrigating material for root canal has not been studied . Hence, the antimicrobial efficacy of the alcoholic extract of Rhamnus prinoides as an irrigation material against E. faecalis was evaluated in comparison with the 2.5% sodium hypochlorite (NaOCL) solution used for root canals of permanent teeth. Methods: A total of 30 single-rooted human permanent teeth were thoroughly cleaned, shaped, and disinfected. Then, each tooth was subjected to a two-week infection with Enterococcus faecalis at 37 °C . Afterward, the samples were divided into three groups (10 teeth per group): 0.9
... Show MoreObjectives: To assess the relation between breast cancer & blood groups, identify the importance of women
age group and the relation of age with breast cancer.
Methodology: The study was performed on (115) women who were diagnosed with breast cancer in different
stages of disease and different ages. Blood samples were taken from them to demonstrate their blood groups and
(20) fresh tumor tissue samples were obtained; the tumor tissue used as a source of lectin for hemagglutinate
with erythrocyte of different blood groups. The study conducted at Baghdad Teaching Hospital and Radiation &
Nuclear Medicine Hospital from January, 2007 through June 2007.
Results: The study shows that the highest percentage of women