Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents

Habib, Nargues S.,Soliman, Raafat,El-Tombary, Alaa A.,El-Hawash, Soad A.,Shaaban, Omaima G. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12

In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5-d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7 -substituted-5-methyl-3-phenylthiazolo[4,5-d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.

Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents

Nargues S. Habib,Raafat Soliman,Alaa A. El-Tombary,Soad A. El-Hawash,Omaima G. Shaaban 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12

In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5- d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine- 2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7-substituted-5-methyl-3-phenylthiazolo[4,5- d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d] pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5- methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.

MDM2 Expression in Serous and Mucinous Epithelial Tumours of the Ovary

Abdelaal, Shereen E,Habib, Fahima M,el Din, Amina A Gamal,Gabal, Samia M,Hassan, Nabila S,Ibrahim, Nihad A Asian Pacific Journal of Cancer Prevention 2016 Asian Pacific journal of cancer prevention Vol.17 No.7

Background: Different types of cancer exhibit abnormalities in cell cycle regulators. The murine double minute-2(MDM2) cell cycle regulator is a proto-oncogene that negatively regulates the P53 tumour suppressor gene. Surface epithelial tumours constitute approximately two thirds of ovarian neoplasms. Each histologic type can be classified as benign, borderline and malignant. This study aimed to examine immunohistochemical expression of the MDM2 protein in ovarian serous and mucinous epithelial tumours (benign, borderline and malignant). Materials and Methods: This study included forty five ovarian tumours, subdivided into fifteen cystadenomas (5 serous and 10 mucinous), fifteen borderline tumours (11 serous and 4 mucinous) and fifteen cystadenocarcinomas (9 serous and 6 mucinous). Paraffin sections were stained with haematoxylin and eosin for histopathologic study, and with mouse monoclonal anti-MDM2 antibody for immunohistochemistry. Results: MDM2 positivity was detected in 28.9% of the studied ovarian tumours. All benign tumours were negative and positivity was significantly higher in malignant than borderline tumours (P value of chi-square test =0.000). Significantly, all MDM2 positive mucinous tumours were malignant with no positive mucinous borderline tumours. Malignant tumours showed positive MDM2 expression in 83.3% of mucinous type and in 55.6% of serous type. Borderline serous tumours showed negative MDM2 in 72.7% of cases (P value of Z test =0.04). Conclusions: Alterations in the expression of the cell cycle regulator (MDM2) occur early in the process of tumourigenesis in serous and mucinous ovarian tumours. We suggest that MDM2 may be used in those tumours as a marker for risk stratification and identification of cases with cancer development and progression. We recommend further studies on MDM2 immunohistochemistry, in conjunction with adjuvant methods as DNA ploidy and FISH gene amplification, focusing on the mucinous tumours and differentiating between the three tumour categories, benign, borderline and malignant.

Anti-cancer Effect of Hyoscyamus muticus Extract via Its Activation of Fas/FasL-ASK1-p38 Pathway

Amer Ali Abd El-Hafeez,Hala Mohamed M. Marzouk,Mohamed A. A. Abdelhamid,Hazim O. Khalifa,Tamer H. A. Hasanin,Ahmed G. K. Habib,Fatma Mahmoud Abdelwahed,Fatma M. Barakat,Eslam M. Bastawy,Eman M. B. Abd 한국생물공학회 2022 Biotechnology and Bioprocess Engineering Vol.27 No.5

Hyoscyamus muticus L. is a traditional medicine used as antispasmodic and sedative. Herein, we aimed to determine the phytochemical constituents and for the first time its anti-cancer activities. The phytochemical constituents of the different extracts were evaluated by calorimetric methods. The anti-cancer activities of the extracts were tested against leukemia, breast, renal, and prostate cancers cell lines. 4, 6-Diamidino-2-phenylindole (DAPI) staining, flow cytometric analysis, knockdown of ASK1, and reactive oxygen species (ROS) production were evaluated to clarify the mechanism of action. Phytochemical screening confirmed the presence of wide range of phytoconstituents. Hyoscyamus muticus methanolic extracts (HMME) showed the highest anti-cancer activities against leukemia, breast, renal, and prostate cancers as compared to ethanol and aqueous extracts. Specifically, HMME exerted cytotoxic effect against the MDA-MB-231 and MDA-MB-468 triple-negative breast cancer (TNBC) cell lines with IC50 values of 8.75 and 7.25 μg/mL, respectively. Mechanistically, DAPI staining and flow cytometric analysis revealed that HMME induces apoptosis via the death receptor, FAS, but not the mitochondrial pathway. Moreover, ASK1 and p38 were rapidly activated in response to HMME, and knockdown of ASK1 by a small interference of RNA specific to Ask1 attenuated p38 and caspase-3 activation and suppressed apoptosis, implying that HMME-induced apoptosis relies on the ASK1-p38-caspase-3 pathway. Furthermore, we confirmed that cellular ROS generation was a critical mediator in HMME-induced apoptosis because the ROSscavenger N-acetyl cysteine significantly decreased the phosphorylation of ASK1 and HMME-induced apoptosis. Our results confirmed HMME cytotoxic effects in TNBCs via ROS-dependent activation of the Fas/FasL-ASK1-p38 axis.

Cap-Assisted Technique versus Conventional Methods for Esophageal Food Bolus Extraction: A Comparative Study

Mahmoud Wahba,Ghada Habib,Ahmed El Mazny,May Fawzi,Mohamed A. Elfeki,Seham Sabry,Mahommad ELbaz,Sayed M Seif El Nasr 대한소화기내시경학회 2019 Clinical Endoscopy Vol.52 No.5

Background/Aims: Food bolus impaction is the most common form of esophageal foreign body impaction observed in adults. Clinicalguidelines recommend using the push technique or retrieval methods in such cases. The push technique can cause injuries in certainclinical situations. Notably, conventional retrieval methods are time and effort consuming. Cap-assisted endoscopic extraction of animpacted food bolus is an easy and effective technique; however, more data are needed for its validation. This study compared the capassistedextraction technique with conventional methods. Methods: This prospective observational multicenter study compared the success and en bloc removal rates, total procedure time, andadverse events in both techniques.. Results: The study included 303 patients who underwent food bolus extraction. The push technique was used in 87 patients (28.7%) anda retrieval procedure in 216 patients (71.3%). Cap-assisted extraction was performed in 106 patients and retrieval using conventionalmethods in 110 patients. The cap-assisted technique was associated with a higher rate of en bloc removal (80.2% vs. 15%, p<0.01), shorterprocedure time (6.9±3.5 min vs. 15.7±4.1 min, p<0.001), and fewer adverse events (0/106 vs. 9/110, p<0.001). Conclusions: Cap-assisted extraction showed no adverse events, higher efficacy, and a shorter procedure time compared withconventional retrieval procedures.

Zinc doping effects on the microstructural, electrical and optical properties of nanostructured ZnxBi2-xS3 (0≤x≤0.09) thin films grown by ultrasonic spray pyrolysis

Bouachri M.,Oubakalla M.,El-Habib A.,Guerra Carlos Díaz,Shaili H.,Fernández Paloma,Zimou J.,Nouneh K.,Fahoume M. 한국물리학회 2023 Current Applied Physics Vol.54 No.-

Zinc-doped bismuth sulfide (Bi2-xZnxS3) nanocrystalline thin films were deposited on glass substrates by using an ultrasonic spray pyrolysis (USP) technique and their structural, morphological, electrical and optical properties experimentally addressed. X-ray diffraction (XRD) and micro-Raman spectroscopy have confirmed the generation of a single-phase polycrystalline orthorhombic material. The crystallite size and micro-deformation of the films was found to depend on the dopant concentration. The surface appears condensed and dense with a uniform spatial grain distribution, as revealed by scanning electron microscopy (SEM) images. Energy dispersive X-ray spectroscopy (EDS) studies revealed a certain Bi deficiency in both undoped and Zn-doped films. When the nominal Zn doping concentration increases from x = 0 to x = 0.09, the crystallite size decreases from 30 to 21 nm. The optical band gap of the films increased from 1.62 to 1.65 eV with Zn content increasing up to x = 0.06, then reducing to 1.58 eV for the maximum Zn content. Optical measurements showed a high absorption coefficient (α > 104 cm−1) in the visible and near-infrared ranges. The Urbach energy followed a similar behavior as a function of doping concentration. The electrical conductivity as well as the sheet carrier mobility of the Bi2-xZnxS3 films increase sharply by increasing the Zn content up to x = 0.06. For this doping concentration, mobility reaches 1.37 × 105 cm2/Vs while keeping carrier concentration above 1017 cm−3. Our experimental results provide strong evidence that Zn-doping is a suitable method to increase Bi2S3 light-harvesting efficiency in solar cell devices.

Investigation of Physical and electrochemical properties of Ni doped CeO2 Thin films: DFT calculation

Zimou J.,Nouneh K.,Talbi A.,El Gana L.,Hsissou R.,El Habib A.,Ahmoum H.,Briche S.,El Jouad Z.,Beraich M.,Addou M. 한국물리학회 2021 Current Applied Physics Vol.31 No.-

Undoped and Ni-doped thin films of cerium dioxide have been deposited by spray pyrolysis technique on the glass substrate at the optimized temperature (450 ± 5) ◦C. Thin films Ce1-xNixO2 doped by different concentrations of Ni was characterized by X-ray diffraction. Raman analysis showed a peak at 461 ± 1 cm 1 position for the undoped film, which corresponds to the active mode (F2g mode) of the cubic fluorite structure. SEM images showed that the particles have a uniform spherical shape. EDS data have confirmed all elements (Ce, Ni and O) existence. Optical properties of samples show a decrease in band gap energy with increasing the nickel rate. Cyclic voltammetry indicates that the storage capacity of samples increases as the Ni rate increases. The EIS of CeO2/ITO electrodes displays a small semicircular at high frequency. The theoretical results obtained using WIEN2k match well with the experimental ones.