Preferred Language
Articles
/
bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
...Show More Authors

The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple  drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed  towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of  two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis  of the target compounds was  accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed  that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug  selectively  into the cancer cells to be hydrolyzed by enzymes that are elevated in  tumor tissues compared with normal tissues .

Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Wed Nov 24 2021
Journal Name
International Journal Of Drug Delivery Technology
Comparison among the Synthesis of Some Azomethine Derivatives by Classical and Non-classical Methods
...Show More Authors

الوصف In this time, most researchers toward about preparation of compounds according to green chemistry. This research describes the preparation of 2-fluoro-5-(substituted benzylideneamino) benzonitrile under reflux and microwave methods. Six azomethine compounds (B1-6) were synthesized by two methods under reflux and assisted microwave with the comparison between the two methods. Reflux method was prepared of azomethine (B1-6) by reaction of 5-amino-2-fluorobenzonitrile with some aldehyde derivatives with (50–100) mL of absolute ethanol and some quantity of GAA and time is limited between (2–5) hours with a yield between (60–70) percent with recrystallization for appropriate solvents. But the microwave-assisted method was synthe

... Show More
Scopus (6)
Scopus
Publication Date
Sun Nov 06 2022
Journal Name
Hiv Nursing
Synthesis, Structural Characterisation and Biological Activity of New Mannich Compounds Derived from Cyclohexanone Moiety
...Show More Authors

The formation and structural investigation of three new Mannich bases are reported. The synthesis of these compounds was accomplished via a multicomponent one-pot reaction using CaCl2 as a catalyst. The reaction of the benzaldehyde, m-bromoaniline and cyclohexanone or 4-methylcyclohexanone resulted in the formation of L1 and L3, respectively. The synthesis of L2 was achieved by mixing benzaldehyde, o-bromoaniline and cyclohexanone. The isolated compounds were characterised using a range of analytical and spectroscopic techniques. These include; NMR (1H and 13C-NMR), ESMS, FTIR, electronic spectroscopy, microanalyses and melting points. The NMR data for L1 and L2 indicated the presence of one isomer in solutions, on the NMR time scale. How

... Show More
Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and biological activity of new esters derived from D-fructose-containing isoxazole moiety
...Show More Authors

Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield

... Show More
Publication Date
Sun Jan 01 2023
Journal Name
Dental Hypotheses
Revolutionizing Systematic Reviews and Meta-analyses: The Role of Artificial Intelligence in Evidence Synthesis
...Show More Authors

View Publication
Scopus (20)
Crossref (11)
Scopus Clarivate Crossref
Publication Date
Thu Nov 01 2018
Journal Name
Colloids And Surfaces B: Biointerfaces
Green synthesis of silver nanoparticles using turmeric extracts and investigation of their antibacterial activities
...Show More Authors

View Publication
Scopus (333)
Crossref (336)
Scopus Clarivate Crossref
Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
synthesis morpholine diamide by curing some aromatic
...Show More Authors

in this work many amide polymers were prepared according to the modification reaction of polyacryloyl chloride or poluacrulic acid with different primary amines to mesuringninizing hormone were investgaited prior tq surgery in 10 postmenopaisal women with benign and 10 postmenopausal women with maliganant healthy

View Publication Preview PDF
Publication Date
Wed Jul 11 2018
Journal Name
Iraqi Journal Of Agricultural Sciences
SYNTHESIS OF RAYON FROM DATE PALM FRONDS ‫
...Show More Authors

The artificial silk (Rayon) was produced from the fronds of date palms which was taken from date palm trees (type Al-Zahdi) from the Iraqi gardens. Two main parts of the frond, namely leaves and stalks were used in this study to produce rayon. The palm fronds were converted into a powder of 90-180 micrometers. Major steps were used to produce rayon; delignification, bleaching and finally dissolution. Modified organosolv method which uses organic solvent method was applied to remove high lignin content. Three variables were studied in the delignification process: temperature, the ratio of ethanol to water and digestion time. The results showed that the best percent of lignin removal was (97%) which occured at; digestion time (80 minutes), te

... Show More
Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Green Chemistry Synthesis of Modified Silver Nanoparticles
...Show More Authors
Abstract<p>The important aspect of this unconventional approach is that eco-friendly, commercially available and straight forward method was used to prepared Silver Nanoparticles by using AgNO3 and curcumin solution as agent factor. The (TEM), (XRD), and (FTIR) was used to characterise these silver nanoparticles (AgNPs). Two types of bacterial isolates were used to indicate the antibacterial activity silver nanoparticles which prepared by curcumin solution, Gram negative like (Escherichia Coli E. Coli), & Gram positive (Stapha Urous). The results exhibit that silver nanoparticles synthesized by curcumin solution has effective antibacterial activities.</p>
View Publication
Scopus (18)
Crossref (11)
Scopus Crossref
Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Synthesis of some polyimides by different methods
...Show More Authors

in this work the polymides were prepared as rthemally stable polymers by diffrent ways

View Publication Preview PDF
Crossref
Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis of some Heterocyclic Compounds Derived from
...Show More Authors

The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending u

... Show More
View Publication Preview PDF
Crossref