Many previous investigations have found quercetin to be a powerful antioxidant and antitumor flavonoid, but its poor bioavailability has limited its use. This current study investigated the effects of two newly synthesized Quercetin Schiff bases containing 2-amino thiadiazole-5-thiol (Q1), and its benzyl derivatives (Q2) on MCF-7 human breast cancer cells. Cell viability and apoptosis were assessed to determine the toxic effects of Q1 and Q2. Cytotoxicity valuation showed that both compounds inhibited MCF-7 cell growth, and lactate dehydrogenase (LDH) activity increased in a dose-dependent aspect compared to the control group. Comet assay results observed that Q1 and Q2 induce more serious DNA damage than the control (untreated cell); however, in all curried experiments, Q2 showed higher effects than Q1. Hence two synthesized quercetin Schiff bases can take action as a promising anticancer agent. Keywords: quercetin derivatives, Schiff base, breast cancer, MCF-7 Cytotoxic.
With the study of synthesizing new organic compounds and exploring biological potency. Aryldiazenyl derivatives (2-5) were carried out by coupling of diazonium salt of 4-aminoacetophenone (1) and miscellaneous active methylene compounds such as: acetylacetone, ethyl cyanoacetate, dimedone or methyl acetoacetate. Moreover substituted 1,2,3-triazole (7-9) were synthesized by the cyclization of 1-(4-azidophenyl) ethanone (6); (which was obtained by coupling of diazonium salt (1) with sodium azid); with acetylacetone, methyl acetoacetate or methyl cyanoacetate, respectively. The structures of the prepared compounds were promoted by IR, H1NMR and UV/Visible spectra. Further, they were examined in vetro for antibacterial activity against five str
... Show MoreBy unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.
Background: Breast cancer is the most frequently diagnosed malignancy and the second leading cause of mortality among women in Iraq forming 23% of cancer related deaths. The low survival from the disease is a direct consequence to the advanced stages at diagnoses. Aim: To document the composite stage of breast cancer among Iraqi patients at the time of diagnosis; correlating the observed findings with other clinical and pathological parameters at presentation. Patients and Methods: A retrospective study enrolling the clinical and pathological characteristics of 603 Iraqi female patients diagnosed with breast cancer. The composite stage of breast cancer was determined according to UICC TNM Classification System of Breast Cancer and the Ameri
... Show MoreSchiff bases (Sh1-Sh3) have been synthesized (p-aminophenol) was condensed with different aromatic aldehyde in ethanol inthe presence of glacial acetic acid as catalyst. These Schiff bases on treatment with monochloroacetyl choride gave 3-chloro-1-(4-hydroxyphenyl)-4-(substituted)azetidin-2-one(Az4-Az6), with αmercaptoacetic acid gave 3-(4-hydroxyphenyl)-2-( substituted)thiazolidin-4-one (Th7-Th9) and with anthranilic acid gave 3-(4-hydroxyphenyl)-2(substituted)-2,3-dihydroquinazolin-4(1H)-one (Qu10-Qu12). The purity of the derivatives was confirmed by TLC. The some compoundsidentify by (FT-IR and1H, 13C-NMR) data. Some of derivatives were evaluated activity against several microbesto determine ability to inhibit bacterial in some h
... Show MoreA new series of Sulfamethoxazole derivatives was prepared and examined for antifibrinolytic and antimicrobial activities. Sulfamethoxazole derivatives bear heterocyclic moieties such as 1,3,4-thiadiazine {3}, pyrazolidine-3,5-diol {4} 6-hydroxy-1,3,4-thiadiazinane-2-thione {5} and [(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl] {8}. Their structures were elucidated by spectral methods (FT-IR, H1-NMR). Physical properties are also determined for all compound derivatives. Recently prepared compounds were tested for their antimicrobial activity in the laboratory. Each screened compound showed good tendency to moderate antimicrobial activity.
Leishmania 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.
Breast cancer is the second most common cancer in women world. Multiple Cytokines appear to have a dominant role in human breast cancer formation. Estimation of the in situ expression of IL-6 and IL-1β in breast cancer patients. A sixty patients with breast cancer BC were divided into two clinical subgroups, (30) with malignant breast cancer MBC and (30) with benign breast tumor as a control group according to histological examination. In situ hybridization technique used for detection of IL-6 and IL-1β mRNA sequence in two groups. The results showed that percentages of mRNA expression of IL-6 and IL-1β were in (≥ 11-50%) for malignant breast cancer. This research also investigated that (73.3%) of beni
... Show MoreThe last few years witnessed great and increasing use in the field of medical image analysis. These tools helped the Radiologists and Doctors to consult while making a particular diagnosis. In this study, we used the relationship between statistical measurements, computer vision, and medical images, along with a logistic regression model to extract breast cancer imaging features. These features were used to tell the difference between the shape of a mass (Fibroid vs. Fatty) by looking at the regions of interest (ROI) of the mass. The final fit of the logistic regression model showed that the most important variables that clearly affect breast cancer shape images are Skewness, Kurtosis, Center of mass, and Angle, with an AUCROC of
... Show MoreLeishmania species are the causative agent of a tropical disease known as leishmaniasis. Previous studies on the old world species Leishmania major, showed that the amastigotes form which resides inside the macrophage of the vertebrate host, utilize host’s sphingolipids for survival and proliferation. In this study, gene expression of serine palmitoyltransferase (SPT) subunit two (MmLCB2) of the mouse macrophage cell line (RAW264.7), which is the first enzyme in the de novo sphingolipid biosynthesis, was detected in both infected and non-infected macrophages. This was detected under condition where available sphingolipid was reduced, with the new world species Leishmania mexicana. Results of qPCR analysis showed that there was no differen
... Show MoreThis study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.
These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linke
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