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.
The amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c] , which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid .Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl[IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V] , However , reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives[VI.VII]a-c. The structure of these compounds was characterized from their melting point , FTIR spectroscopy and elementalanalysis
Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf
... Show MoreLeishmania is auxotroph to folic acid,antifolates drug inhibit the synthesis and conversion of folate derivatives. In this study, cytotoxic effect of methotrexate was investigated on the procyclic promastigotes proliferation of L. donovani. The results showed a significant (p ≥ 0.05) difference in growth of treated groups at high concentrations (1000, 500, 250, 125.5) μM after 24, 48 hrs., while at 72 hrs. significant difference was observed at all concentration. The IC50 values was measurable after 24, 48 and 72 hrs. and it was 174.238, 52.283 and 109.175 μM, respectively. The present study showed the cytotoxic effect of methotrexate on the proliferation of promastigotes of the visceral type of Leishmania.
In this paper, an attempt was made to measure and interpret the impact of several variables on global maritime transport, including: OECD industrial productions, high growth rates of some developing countries, and growth in world GDP. These variables contribute to higher rates of maritime transport revenues of 800 billion dollars annually; in the form of numerical sequences. The dry canal in Iraq was assumed to transfer 99 million tons of goods annually. This was made sure through the economic feasibility of the difference between maritime and land transport through railways. The effect of geographical and anthropological nature of Iraq on this project was studied too. Our findings indicated that the project will not drive growth
... Show MoreIn the current study, gold nanoparticles were made using Acinetobacter baumannii broth culture. UV-vis, FTIR, XRD, FESEM, AMF, and zeta potential measurements were also used to study the properties of the Ab-AuNPs. The average was 66 nm, ranging from 20 to 90 nm. The examination results proved that the Ab-AuNPs are semi-spherical and varied from 20 to 90 nm, with an average of 66 nm.
MTT assay on the breast cancer cell line MCF-7 confirmed the anticancer activity in vitro. Cancer cells showed an important cytotoxic activity of Ab-AuNPs. The breast. Cancer cell. Line.MCF-7 but ineffective against the normal.cell line.MCF-10. The IC50 values of Ab-AuNPs were at 11.45 μg ml-1. The results proved that Ab-
... Show MoreBoth methotrexate and vitamin D3 are used in combination for the treatment of various diseases. The aim of this study is to highlight the effect of vitamin D3 on methotrexate-induced jejunum damage using biochemical and histopathological studies. Seven groups of both sexes of rats were selected and treated as follows: (Group I and Group II) : control 1,control 2 (I.P normal saline) daily for 14 and 21 days respectively ; (Group III and Group IV) :vitamin D3 groups (500 IU/rat/day) orally for 14 and 21 days, respectively;(Group V): once daily dose of methotrexate 20mg/kg, I.P injected for 4 days;(Group VI):vitamin D3 (500 IU/rat/day) once daily for 14 days and methotrexate (20 mg/kg I.P) injected only at day 10;.(Group
... Show MoreBiomarkers such as Interleukin-6 (IL-6), Procalcitonin (PCT), C-reactive protein (CRP) and Neutrophil-Lymphocyte Ratio (NLR) have a role in the pathogenesis of severe coronavirus disease 2019 (COVID-19). The aim of this study was to explore the differences between serum levels of such biomarkers in severe and non-severe COVID-19 cases and compare them with normal people and to evaluate the sociodemographic variables and chronic diseases effect on the severity of COVID-19. The study included 160 subjects, divided into two groups, a case group of 80 patients, and a control group of 80 normal persons. The case group was divided into two subgroups: 40 severe COVID-19 patients and 40 patients with non-severe disease. Blood IL-6 was asses
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