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
Sat Dec 30 2023
Journal Name
Journal Of The College Of Education For Women
Salience and Erasure in Environmental Advertisements: An Ecolinguistic Study
...Show More Authors

Ecolinguistics is a twofold field in which ecology and language are its two major concerns. That is, this field is concerned with the way through which our thoughts, ideologies and the like influence the environment. The present study aims at analyzing (6) constructive and destructive environmental advertisements to find out how the techniques of erasure and salience operate in these types of advertisements. It studies the linguistic expressions that achieve these techniques in the constructive and destructive advertisements. The qualitative and quantitative methods are exploited in the current study. Analyzing (6) constructive and destructive environmental advertisements in accordance with Stibbe’s (2015) model of salience and erasure

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Sep 01 2020
Journal Name
Journal Of Coloproctology
Epidemiological and prognostic single center study of anal carcinoma
...Show More Authors
Abstract<p> Background Anorectal carcinoma includes the anal margin, the anal canal, and the lower rectum. The incidences of anal tumors represent 1.4 % of all gastrointestinal tumors.</p><p> Patients and methods Our study is retrospective and was conducted at Baghdad Medical City. Patient’s data were collected from the medical records through a predesigned sheet that included the following information: demographic data, medical history, past-history, presenting symptoms, pathological data, and treatment details.</p><p> Results The median age was 49 years. As regard tumor extension, 85.71 % of patients had anal disease, while anorectal cancer was encount</p> ... Show More
View Publication
Scopus (8)
Crossref (6)
Scopus Crossref
Publication Date
Sat Apr 01 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of 3 - 3 - gem - di - C -Nitromethyl Nucleoside Analogues of Possible Biological Activity
...Show More Authors

Synthesis of new nucleoside analogues of the type : 3¢ , 3¢ - gem – di – C – nitromethly , expected to have useful application in the chemotherapeutic treatment of AIDS , cancer and microbial infections. The synthesis involved the condensation of the appropriate sugar derivative ( i.e . 3¢ , 3¢ –  gem – di – C – nitromethly – 1–  ribofuranose ) with nitrogen bases , such as , uracil and theophllin following a multi step scheme starting from diacetone golucose (1) (scheme 1) .The prepared compound were identified by spectroscopic methods ; ir , mass , 1H and 13C nmr.

View Publication Preview PDF
Crossref
Publication Date
Sun May 28 2017
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci
Synthesis of Some New Heterocyclic Fused Rings Compounds Based on 5-Aryl-1,3,4-Oxadiazole
...Show More Authors

The work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4- chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compo

... Show More
Preview PDF
Publication Date
Wed Jun 26 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Acetylenic Derivatives of a Substituted 1, 3, 4-Thiadiazole as Antibacterial Agents
...Show More Authors

View Publication Preview PDF
Scopus (2)
Scopus Crossref
Publication Date
Mon Sep 25 2017
Journal Name
Bn Al-haitham Jour. For Pure & Appl. Sci.
Synthesis of Some New Heterocyclic Fused Rings Compounds Based on 5-Aryl-1,3,4-Oxadiazole
...Show More Authors

The work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4-chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compound (3)

... Show More
Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
The Effect of Temperature on the Synthesis of Nano-Gamma Alumina Using Hydrothermal Method
...Show More Authors

Nano gamma alumina was prepared by double hydrolysis process using aluminum nitrate nano hydrate and sodium aluminate as an aluminum source, hydroxyle poly acid and CTAB (cetyltrimethylammonium bromide) as templates. Different crystallization temperatures (120, 140, 160, and 180) 0C and calcinations temperatures (500, 550, 600, and 650) 0C were applied. All the batches were prepared at PH equals to 9. XRD diffraction technique and infrared Fourier transform spectroscopy were used to investigate the phase formation and the optical properties of the nano gamma alumina. N2 adsorption-desorption (BET) was used to measure the surface area and pore volume of the prepared nano alumina, the particle size and the

... Show More
View Publication Preview PDF
Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines
...Show More Authors

A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound

... Show More
View Publication Preview PDF
Scopus (20)
Crossref (7)
Scopus Clarivate Crossref
Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines
...Show More Authors

A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound

... Show More
Scopus (20)
Crossref (7)
Scopus Clarivate Crossref
Publication Date
Sat Jan 25 2025
Journal Name
Indonesian Journal Of Chemistry
Synthesis of CuO Nanoparticles from Copper(II) Schiff Base Complex: Evaluation via Thermal Decomposition
...Show More Authors

Copper oxide (CuO) nanoparticles were synthesized through the thermal decomposition of a copper(II) Schiff-base complex. The complex was formed by reacting cupric acetate with a Schiff base in a 2:1 metal-to-ligand ratio. The Schiff base itself was synthesized via the condensation of benzidine and 2-hydroxybenzaldehyde in the presence of glacial acetic acid. This newly synthesized symmetric Schiff base served as the ligand for the Cu(II) metal ion complex. The ligand and its complex were characterized using several spectroscopic methods, including FTIR, UV-vis, 1H-NMR, 13C-NMR, CHNS, and AAS, along with TGA, molar conductivity and magnetic susceptibility measurements. The CuO nanoparticles were produced by thermally decomposing the

... Show More
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref