Preferred Language
Articles
/
bijps-563
Cephalothin as a Carrier of 6-Mercaptopurine for Targeting Cancer Tissues
...Show More Authors

A lower extracellular pH is one of the few well-documented physiological differences between tumour and normal tissues. On the other hand, elevated glutathione (GSH) level has been detected in many tumours compared with healthy surrounding tissues. The compound II: 3-(9H-purin-6-yl-thio) carbonothionyl methyl-8-oxo-7-(2-thiophen-2-yl) acetamido-5-thia-1-azabicyclo-4-octo-ene-carboxylic acid was a cephalothin derivative contain 6-mercaptopurine (6-MP). Compound II react with general base catalysis in slightly acidic pH or with sulfhydryl nucleophiles to release the chemotherapeutic drug 6-MP. The generation of compound II was accomplished following multistep reaction procedures. The structure of compound II and its intermediate was confirmed by their melting point, infrared spectroscopy, CHN and NMR analysis. The hydrolysis of compound II in aqueous buffer solution of pH 6 and in the presence of GSH at pH 7.4 was studied. The partition coefficient (PC) of compound II was also determined. Compound II has acceptable rate of hydrolysis at slightly acidic medium pH 6 (t1/2 = 56.34 min.) and 80% of compound II had been converted to 6-MP within 30 min in the presence of GSH. And the compound has acceptable stability at pH 7.4(t0.5=639.65 min.) and the rate of hydrolysis was effected by change the buffer concentration.  This compound can selectively deliver 6-MP into the tumour tissues which have acidic pH or elevated GSH level. Compound II had an improved PC value of 12.23 compared to 1.22 for free drug 6-MP confirming higher lipophilicity.

Key words: 6-mercaptopurine, cancer, prodrug, targeting

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Wed Jun 09 2021
Journal Name
International Journal Of Environmental Science And Technology
Water quality index toward a reliable assessment for water supply uses: a novel approach
...Show More Authors

View Publication
Scopus (23)
Crossref (22)
Scopus Clarivate Crossref
Publication Date
Wed Nov 21 2018
Journal Name
International Journal Of Control, Automation And Systems
Design and Stability Analysis of a Fractional Order State Feedback Controller for Trajectory Tracking of a Differential Drive Robot
...Show More Authors

View Publication
Scopus (22)
Crossref (19)
Scopus Clarivate Crossref
Publication Date
Mon Feb 15 2021
Journal Name
Systematic Review In Pharmacy
Colorimetric Determination Of Sitagliptin As An Oxidation Derivative Of Ninhydrin
...Show More Authors

A sensitive and accurate colorimetric method was developed for the determination of the Sitagliptin phosphate monohydrate, here and after will be named Sitagliptin, in its pure and pharmaceutical form. The suggested approach is based on boosting the sensitivity of the traditional spectrometric methods by derivatizing Sitagliptin into a colored product that absorbs the visible spectrum at 573 nm. The proposed method has effectively improved the sensitivity and the limit of detection for the analysis of Sitagliptin. A linear calibration curve was obtained over the concentration range of 0.1-10 μg/ml with a correlation coefficient of 0.9983. The calculated recovery was within the range of 98.98–100.11%. While the limit of detection LOD and

... Show More
Preview PDF
Publication Date
Mon Jan 01 2018
Journal Name
Organic & Biomolecular Chemistry
Small-molecule anticancer agents kill cancer cells by harnessing reactive oxygen species in an iron-dependent manner
...Show More Authors

In the course of generating a library of open-chain epothilones, we discovered a new class of small molecule anticancer agents that has no effect on tubulin but instead kills selected cancer cell lines by harnessing reactive oxygen species in an iron-dependent manner.

View Publication
Scopus (12)
Crossref (13)
Scopus Clarivate Crossref
Publication Date
Mon Jan 01 2024
Journal Name
Iraqi Journal Of Hematology
Provisional diagnosis of clinically significant hemoglobinopathies and decision on suitability for marriage as part of the premarital screening program in Iraq: Iraqi Society of Hematology Guidelines
...Show More Authors

View Publication
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Women's Knowledge about Risk Factors and Early Detection of Breast Cancer at Ibn Rushd College of Education in Baghdad University
...Show More Authors

Objective: Evaluation of women's knowledge about risk factors and early detection of breast cancer at
Ibn Rushd college of education in Baghdad University.
Methodology: The study sample included (184) women in the Ibn Rushd College / University of
Baghdad, whose age ranged between (17-58) years. Data were collected through a structured
questionnaire prepared by the National Cancer Research Center which were answered during a scientific
symposium about breast cancer. The score was calculated by correcting the results of the answer, giving
one score for each correct answer and then estimating the level of knowledge and inputting all data in a
statistical program.
Results: The results showed limited level of women's

... Show More
View Publication Preview PDF
Publication Date
Tue Jan 01 2019
Journal Name
In Indian Journal Of Public Health Research And Development
The Significance of p53, Bcl-2, and HER-2/neu Protein Expression in Iraqi Females Breast Cancer Cell Line (AMJ13)
...Show More Authors

-----

Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Prevalence of UGT1A1*93 and ABCC5 Polymorphisms in Cancer Patients Receiving Irinotecan-Based Chemotherapy at Al-Najaf Al-Ashraf
...Show More Authors

Irinotecan (CPT-11) is a semisynthetic derivative of the antineoplastic agent camptothecin used in a wide range as an anti-cancer agent in many solid tumors because of its cytotoxic effect through the interaction with the topoisomerase I enzyme. The major limiting factors for irinotecan treatment are its association with potentially life-threatening toxicities including neutropenia and acute or delayed-type diarrhea, results from distinct interindividual and interethnic variability due to gene polymorphism.

This is a cross sectional pharmacogentics study was conducted on 25 cancer patients to estimate the prevalence of UGT1A1*93 and ABCC5 allele single nucleotide polymorphism (SNP) in Iraqi cancer patients treated with irinotecan

... Show More
View Publication Preview PDF
Scopus (4)
Scopus Crossref
Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
The Effect of Silybum marianum L. aquatic crude extracts on the cancer cell lines and normal cell line in vitro
...Show More Authors

The aquatic crude extract of Silybum marianum dry grains prepared by melting them in distil water by the method of soak and shake. The effect of Silybum marianum crude extract studied in vitro on three tumor cell line the Hep-2, AMN-3 and RD for 24, 48 and 72 hours of exposure, and one cell line of normal cells REF for 72 hr exposure. The results showed that the prescence of toxic effect of the aquatic crude extract on the cell lines of Hep-2, AMN-3 and RD at 10 and 100 µg/ ml upto the higher concentrations when they exposed to the extract for 48 hr. as compared with the control treatment, and when the exposure period increased to 72 hr. the toxic effect started at low concentrations (5 and 10 µg/ ml) as compared with the control g

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Mar 02 2014
Journal Name
Baghdad Science Journal
Kinetic and thermodynamic Studies Of Alanine Aminopeptidase(AAP) Isoenzymes I,II Partially Purified From Patient's Urine With Urinary Tract Cancer
...Show More Authors

The activity of Alanine aminopeptidase( AAP ) was measured in the urine of healthy and urinary tract cancer patients , the results showed higher activity of (AAP) in patients compared to healthy . AAP was Purified from the urine of healthy and patients with urinary tract cancer by dialysis and gel filtration (Sephadex G – 50) and two isoenzymes of (AAP) were separated from urine by using ion-exchang resin (DEAE – Sephadex A – 50 ) in previous study. The kinetics studies showed that both isoenzymes I and II obeyed Michaelis – Menton equation . with optimal concentration of alanine-4-nitroanilide as substrate for isoenzymes I and II which was (2 x 10-3 mol/L ). The two isoenzymes obeyed Arrhenius equation up two 37° C and t

... Show More
View Publication Preview PDF
Crossref