ABSTRACT. Through the present work the 3-oxo-N,3-diphenylpropamide derivatives 5a,b were used to synthesize pridine, pyrazole and thiophene derivatives. 3-Phenylisoxazol-5(4H)-one produced from the reaction of ethyl benzoylacetate was used as the key starting compound for different multi-component reactions. The synthesized compounds were evaluated toward Hepatocellular carcinoma HepG2 and cervical carcinoma HeLa cell lines. Compounds 3b, 5b, 7b, 7d, 9c, 9d, 15e, 15f, 16b, 18b, 18e, 18f, 19e and 19f were the most cytotoxic compounds against the tested cell lines. The results obtained in this work encourage further work in the future to produce new cytotoxic compounds.   KEY WORDS: Diphenylpropamide, 3-Phenylisoxazole, Pyran, Pyridine, Cytotoxicity Bull. Chem. Soc. Ethiop. 2023, 37(1), 141-158.                                                              DOI:https://dx.doi.org/10.4314/bcse.v37i1.12

Hepatitis C Virus (HCV) is a major health care concern worldwide. Egypt shows the highest worldwide HCV prevalence. Fibrosis progression is common in HCV and it is the most important prognostic factor in chronic HCV patients. The aim of this study was to investigate changes in some parameters of liver fibrosis progression after successful HCV eradication by direct acting antiviral (DAA) therapy in Egyptian patients. The study included 100 chronic HCV patients. liver stiffness measurement (LSM) was obtained by Transient elastography (TE) or Fibroscan before starting DAA treatment, after the end of 12 weeks of treatment and after achieving sustained virologic response12 (SVR12). Based on baseline LSM, patients were stratified into F2, F3 and F4 groups (METAVIR), F0-F1 patients were excluded. LSM and laboratory data after the end of treatment and after achieving SVR12 was compared with that baseline values in each fibrosis group. Following DAA treatment, all patients achieved SVR12. Mean baseline LSM dropped from 13.5 to 10.1 (kPa) post SVR12; the maximum change occurred in F2 patients 84.3% versus 84.2%, 43.3% in F3, and F4 patients respectively (p<0.001). At baseline, 30 patients were in the F4 group; only 11 patients (43.3%) regressed to noncirrhotic range (<12.5 kPa), while 19 patients (56.7%) were still cirrhotic despite achieving SVR12 (p<0.001). Patients showed significant improvement in platelets count and decreased ALT enzyme levels after achieving SVR12 (p<0.001). So, successful eradication of HCV results in significant LSM improvement; the best improvement occurs in F2 and F3 patients.

ABSTRACT. Benzoylacetone (1) underwent a series of multi-component reactions with aromatic aldehydes and malononitrile or ethyl cyanoacetate to produce the pyran derivatives 4a-f. The latter compounds reacted with malononitrile or ethyl cyanoacetate to yield the condensation products 5a-m. On the other hand, the reaction of 4a-f with either the diazonium salts 6a-c yielded the arylhydrazone derivatives 7a-i. The multi-component reaction of (1) with aromatic adehydes and cyclohexan-1,3-dione produced the  pyran derivatives 9a-c. Compound 1 underwent the Gewald’s reactions with elemental sulfur and malononitrile or ethyl cyanacetate yielding the thiophene derivatives 10a,b. Evaluations of the  synthesized  products were carried out against some selected cancer cell lines and the most active compounds were further evaluated against the seventeen cancer cell lines classified according to the disease. Morphological changes of A549 cell line by the effect of compound 7k was studied using microenvironment of the lung tissue where an excellent results was obtained.   KEY WORDS: Benzoylacetone, Multi-component reactions, Pyran, Thiophene, Arylhydrazone, Cytotoxicity   Bull. Chem. Soc. Ethiop. 2023, 37(2), 405-425.                                                             DOI: https://dx.doi.org/10.4314/bcse.v37i2.12