Background: In spite of all efforts, Non-small cell lung cancer (NSCLC) is a fatal solid tumor with a poor prognosis as of its high metastasis and resistance to present treatments. Tyrosine kinase inhibitors (TKI) such as erlotinib are efficient in treating NSCLC but the emergence of chemoresistance and adverse effects substantially limits their single use. Objective: in this study, the combination treatments of either 2-deoxy-D-glucose (2DG) or cinnamic acid (CINN) with erlotinib (ERL) were tested for their possible synergistic effect on the proliferation and migration capacity of NSCLC cells. Methods: In this study, NSCLC model cell line A549 was used to investigate the effects of single compounds and their combination on cell growth inhibition, clonogenic potential, and migration capacity. Next, the Combination index (CI) and the Dose-Reduction Index (DRI) were determined to determine the nature of the drug’s combination and to measure how many folds the dose could be lowered for each drug in a synergistic combination. Results: the combination treatment demonstrated more significant inhibition of viability of A549 cells compared to individual therapy. Our data show that CINN augments the sensitivity to erlotinib in all doses tested. The combination of 2DG or CINN with erlotinib also reduced the clonogenicity of NSCLC cells up to 67% and 85%, respectively, as compared to the erlotinib single treatment. Furthermore, CINN +ERL decreased the migratory ability of A549 cells by 3-fold and further induced much more apoptotic cell death phenotypes. Conclusion: in summary, co-administration of 2DG or cinnamic acid with erlotinib increases the inhibitory effects of erlotinib on NSCLC cell tumorigenicity and migration.
A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f
... Show MoreThe pandemic SARS-CoV-2 is highly transmittable with its proliferation among nations. This study aims to design and exploring the efficacy of novel nirmatrelvir derivatives as SARS entry inhibitors by adapting a molecular modeling approach combined with theoretical design. The study focuses on the preparation of these derivatives and understanding their effectiveness, with a special focus on their binding affinity to the S protein, which is pivotal for the virus’s access to the host cell. Considering molecular docking aspects in the scope of a study on nirmatrelvir derivatives and S protein, dynamics simulations with 25 nanoseconds of their binding are explored. The study shows that these derivatives might work as effective antivi
... Show MoreFive derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4-thiadiazole, compound E: 2- amino-5-(2-Propanylthio)-1,3,4-thiadiazol) and compound F:2(o-chlorobenzylamino)-5-(2-propanyl thio)-1,3,4 thiadiazol. All prepared compounds were diagnosed by (IR) and (UV) Spectroscopy. All of those compounds were screened for their anti-microbial activity in vitro. The results show that most of the compounds A, B, C exhibited moderate to good activity against Gram-positive bacteria and the same compound exhibit low to moderate activity on most gram-negative bacte
... Show MoreConcentrations 25, 50 and 100 mg of nano-capsules linolenic acid and non-capsulated fatty acid for 1kg of Milk was used for yogurt manufacture. The results showed no significant differences in the ratio of titration acidity and pH values between all processed treatments at the beginning and during of period storage. The treatments was added to it coated omega-3 by nano method were the least exposed to the oxidation process from the non-capsules omega-3, And for shield of The poly lactic acid had a significant role in the protection of alpha-linolenic acid against lipolysis by the formation of a protective layer to protect the acid from the activity of lipases enzymes, and the addition of fatty acid linolenic to milk was determined the gr
... Show Moreليكاند ازو جديد. 4-((3-formyl-2-hydroxyphenyl)diazenyl)-N-(5-methylisoxazol-3-yl)benzenesulfonamide, الليكاند المحضر استعمل لتحضير معقدات من ايونات معادن مختلفة مثل الكروم الثلاثي والمنغنيز الثنائي والحديد الثلاثي والبلاديوم الثنائي بنسب مولية (1:1) ( ليكاند : فلز) نتائج التشخيص للمركبات يتقنيات مطيافية الاشعة فوق البنفسجية الاشعة تحت الحمراء الرنين النووي المغناطيسي البروتوني والكربوني وطيف الكتلة والتحليل الدقيق للعناصر ومحتوى الفلز وال
... Show MoreNew Fourteen compounds were synthesized in four steps. The first step included synthesis of 2-biphenyl fused ring of imidazo(1,2- a)pyrimidine from the reaction of 2-aminopyrimidine and biphenyl phenacyl bromide . The second step was introduced aldehyde group from the reaction of 2-biphenyl fused rings of imidazo(1,2-a)pyrimidine with POCl3 in presence of DMF and CHCl3. 3-Carbaladehyde derivatives of fused imidazo/pyrimidine was reacted with different aromatic amines to afford new Schiff bases. These new 3- imines derivatives was reduced by using sodiumborohydride to yield another new 3-aminomethyl-2-biphenyl imidazo (1,2-a)pyrimidine derivatives in moderate yield .Some new prepared compounds were identified by melting point, FT- IR , 13C-
... Show More2- amino -5- thiol-1,3,4- thiadiazole (S1) was prepared by cyclic locking of thiosemicarbazide in the presence of anhydrous sodium carbonate and CS2. diazotization of (S1) compound gave diazonium salt (S2) that reacts with different activated aromatic compounds to get the following azo compounds ,2 [(4- aminophenyl) diazenyl ] 1,3,4- thiazdiazole-5- thiol (S3) ,2-[4-amino- 1-naphthyl diazenyl] -1,3,4 – thiazdiazole-5-thiol (S4) , 3-amino-4-[(5- mercapto -1,3,4- thiadiazole -2-yl) diazenyl ] phenol(S5) ,1-[(5-mercapto-1,3,4-thiadiazole-2-yl) diazenyl] -2-naphthol (S6) , 5-{[4-(dimethylamino) phenyl] diazenyl}-1,3,4-thiadiazole-2- thiol(S7) ,5-{[4-(diethylamino) phenyl] diazenyl}-1,3,4- thiadiazole-2- thiol(S8) ,2- amino-5-[(5-mercapto-1,3
... Show MoreAbortion is a condition that occurs due to one of the pathological injuries, often one of the members of the TORCH is the real cause. The current study aimed to investigate the impact of toxoplasmosis, HSV-2 infections with abortion, and also, the identification of immunogenetics marker (interleukin-10) that may be associated with abortion. Anti-Toxoplasma IgG, IgM, Herpes simplex virus-2 IgM, human soluble leukocyte antigen class I–G and interleukin10 were estimated by ELISA technique, while the expression of IL-10 gene was investigated by using the real-time PCR. The results showed that among aborted women the rate of anti-Toxoplasma and HSV-2 IgM antibodies occurred within the age groups (21–30) years and (31–40) years 32(100.0%) a
... Show MoreBackground: Verrucous carcinoma (VSCC) is considered as a rare well differentiated carcinoma variant of SCC with no metastatic potential. The aim of this study is to evaluate the Immunohistochemical expression MMP-2, VEGF and D2-40 expression in OSCC and VSCC. Materials and methods: Thirty formalin fixed paraffin embedded tissue blocks of OSCC and another twelve VSCC were collected and Four micrometer thick sections were cut from each block and mounted on positively charged slides and stained immunohistochemically with monoclonal antibodies to MMP-2, VEGF and D2-40. Results: there is no statistical difference between SCC and VSCC regarding the immunoexpression of MMP-2 and VEGF. While the lymphatic vessels density were higher in SCC than V
... Show More