期刊
MINI-REVIEWS IN MEDICINAL CHEMISTRY
卷 19, 期 5, 页码 395-409出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389557518666180820125210
关键词
Cyclohepta[d]pyrimidine; 1,3,4-Oxadiazolyl acyclic C-nucleoside; Haemolytic; Prebiotic; Anticancer; Antimicrobial
Background: New aryl substituted cyclohepta[b]pyridine and cyclohepta[d]pyrimidine derivatives were synthesized. The sugar hydrazones of the synthesized pyridine and pyrimidine compounds were also prepared. Method: In addition, the 1,3,4-oxadiazolyl acyclic (C-nucleoside analogs of the pyridine system were prepared. The hemolytic, prebiotic, anticancer and antimicrobial activities of some of the synthesized compounds were also studied. Compounds 10 and 12 showed high activity against MCF-7, HEPG-2 and HCT-116 cell lines with IC50 at range 3.56-8.55 mu g/mL. In addition, the synthesized condensed thiopyrimidine derivative 10 exhibited more potent bactericidal activity while compound 7 demonstrated potent antifungal activity against Aspergillus niger. Furthermore, the synthetic compounds of the pyrimidine base promoted the growth of lactic acid bacteria. Results: The predicted binding patterns of three of the prepared derivatives as possible antagonists against ER alpha were investigated which showed good binding patterns.
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