Preferred Language
Articles
/
bijps-943
Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
...Show More Authors

Small molecules drug conjugate mutual prodrug design  (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide  bond   ;  represent new interesting approaches for cancer treatment , the component of SMDC intended  for targeting    folate receptor , along with greater conservation  of component until reaching  the target tumor tissue . The  designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were  processed forward  successfully by multistep reaction  procedures , and by Thin Layer Chromatography (TLC) for  preliminary detection of  products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI   possess optimal activity proportional with increased number of 6-MP molecules.

Scopus Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Tue Feb 10 2015
Journal Name
Al-qadisiyah Journal For Science
*Synthesis, spectral studies and antimicrobial evaluation of 6,6--(1,2-benzenediazo) bis (3-amino benzoic acid) complexes with some metal ions
...Show More Authors

The Ligand 6,6--(1,2-benzenediazo) bis (3-aminobenzoicacid) derived from o-phenylenediamine and 3-aminobenzoicacid was synthesized. The prepared ligand was identified by Microelemental Analysis, 1HNMR, FT-IR and UV-Vis spectroscopic techniques. Treatment of the ligand with the following metal ions (CoII, NiII, CuII and ZnII ) in aqueous ethanol with a 1:1 M:L ratio and at optimum pH. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR and UV-Vis, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). H

... Show More
Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Solvent-free synthesis of new chalcone derivatives from 3-nitro phthalic acid and evaluation of their biological activities
...Show More Authors

A theoretical and protection study was conducted of the corrosion behavior of carbon steel surface with different concentrations of the derivative (Quinolin-2-one), namly (1-Amino-4,7-dimethyl-6-nitro-1H-quinolin-2-one (ADNQ2O)). Theoretically, Density Functional Theory (DFT) of B3LYP/ 6-311++G (2d, 2p) level was used to calculate the optimized geometry, physical properties and chemical inhibition parameters, with the local reactivity to predict both the reactive centers and to locate the possible sites of nucleophilic and electrophilic attacks, in vacuum, and in two solvents (DMSO and H2O), all at the equilibrium geometry. Experimentally, the inhibition efficiencies (%IE) in the saline solution (of 3.5%) NaCl were studied using potentiomet

... Show More
View Publication
Scopus (13)
Crossref (4)
Scopus Clarivate Crossref
Publication Date
Tue Jan 01 2019
Journal Name
Baghdad Science Journal
Synthesis of new five-membered hetrocyclic compounds from 2-furfuryl mercaptan derivative and evaluation of their biological activity
...Show More Authors

A theoretical and protection study was conducted of the corrosion behavior of carbon steel surface with different concentrations of the derivative (Quinolin-2-one), namly (1-Amino-4,7-dimethyl-6-nitro-1H-quinolin-2-one (ADNQ2O)). Theoretically, Density Functional Theory (DFT) of B3LYP/ 6-311++G (2d, 2p) level was used to calculate the optimized geometry, physical properties and chemical inhibition parameters, with the local reactivity to predict both the reactive centers and to locate the possible sites of nucleophilic and electrophilic attacks, in vacuum, and in two solvents (DMSO and H2O), all at the equilibrium geometry. Experimentally, the inhibition efficiencies (%IE) in the saline solution (of 3.5%) NaCl were studied using potentiomet

... Show More
Scopus (10)
Scopus
Publication Date
Sat Nov 01 2014
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
Genital Warts in Infants and Children—Re-Evaluation of Podophylline 15% as an Effective Topical Therapy
...Show More Authors

KE Sharquie, AA Noaimi, MN Almallah, Journal of Cosmetics, Dermatological Sciences and Applications, 2014 - Cited by 2

View Publication
Publication Date
Fri Oct 01 2010
Journal Name
Iraqi Journal Of Physics
Evaluation of polyurethane and polyurethane /polyvinyl chloride blend coatings on steel as corrosion protection using EIS technique
...Show More Authors

This paper was aimed to evaluate the polyurethane (PU) and polyurethane/polyvinyl chloride (90 wt. % / 10 wt. %) as organic coating of carbon steel substrate against marine environment (3.5 wt.% NaCl aqueous solution) as a severe corrosion environment . The electrochemical impedance spectroscopy (EIS) and fitting impedance data by ZsimpWin 3.22 software were used to estimate the physical barrier of the samples for different exposure times. Different equivalent electrical circuits were proposed for the physical barrier at different immersion times to get appropriate fitting .Both PU and PU/PVC coatings showed excellent corrosion protection ability for steel .The PU/PVC coating showed better protection and stability than PU coating against

... Show More
View Publication Preview PDF
Publication Date
Wed May 10 2023
Journal Name
Journal Of Planner And Development
Analysis and evaluation of related factors affecting community Participation as a policy to upgrade residential slums area
...Show More Authors

have suffered from deteriorating residential neighborhoods, poor economic, social and urban living conditions of the population and deteriorating the infrastructural and superior services. These problems were the secretions of these cities' rapid urbanization. Based on the principles of sustainable urban planning and in order to achieve adequate opportunities for the lives of the population and provide them with sustainable livelihoods, policies have emerged to upgrade along the lines of community participation and programmes to reform and develop those neighbourhoods, raise their efficiency and make them livable. Thus, the problem of research was identified "The absence of a comprehensive cognitive perception of the most prominent facto

... Show More
View Publication Preview PDF
Publication Date
Sat Jan 25 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Study the Toxicity and Anticancer activity of Some New Amic Acid and Their Derivatives of Mefenamic acid
...Show More Authors

View Publication
Crossref (3)
Crossref
Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-amino-5-chlorobenzothiazole Derivatives Containing Different Types of Heterocyclic as Antifungal Activity
...Show More Authors

Nine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5  then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative

... Show More
View Publication Preview PDF
Scopus (12)
Crossref (4)
Scopus Crossref
Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
...Show More Authors

Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

... Show More
Publication Date
Thu Jul 18 2019
Journal Name
Annals Of Tropical Medicine & Public Health
SURVIVIN TARGETING; AN IN SILICO APPROACH FOR ANTICANCER DESIGN
...Show More Authors

Survivin, a member of inhibitor of apoptosis family is increasingly used as a target for cancer therapy design because it has a key role in cell growth and inhibition of cell apoptosis. Also it can be used as a biomarker for targeting cancer because it is found in almost all cancer but not normal cells. Our strategy was to design (computationally) a molecule to be used as survivin inhibitor. This molecule was named lead10 and was used furthermore to find (virtually) existing drugs with a good survivin inhibition activity.