期刊
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
卷 15, 期 4, 页码 517-526出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520615666150105113946
关键词
Anticancer; antioxidant; docking; pyrrole; structure-activity-relationship; synthesis
资金
- Pharm. Org. Chem. Dep. (Faculty of pharmacy, Helwan University)
A series of N-aryl derivatives of pyrrole and its related derivatives of fused form (namely; tetrahydroindole and dihydroindenopyrroles) were prepared in fair to good yields. The newly synthesized compounds were confirmed using IR, H-1 NMR, Mass spectral and elemental analysis. Tetrahydrobenzo[b] pyrroles Ia-d, 1,4-dihydroindeno[1,2-b] pyrroles IIa,b and pyrroles IIIa-c,e were evaluated for anticancer activity, coinciding with the antioxidant activity; using Di-Phenyl Picryl Hydrazyl (DPPH) tests. The cytotoxicity of the tested compounds (at a concentration of 100 and 200 mu g/mL) was performed against HepG-2 and EACC cell lines. Compounds Ib, d and IIa showed promising antioxidant activity beside their anticancer activity. Docking studies were employed to justify the promising anticancer activity of Ib,d and IIa. Protein kinase (PKase)-PDB entry 1FCQ was chosen as target enzyme for this purpose using the MOLSOFT ICM 3.4-8C program. The docking results of the tested compounds went aligned with the respective anticancer assay results.
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