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A Promising Anti-Cancer and Anti-Oxidant Agents Based on the Pyrrole and Fused Pyrrole: Synthesis, Docking Studies and Biological Evaluation

[ Vol. 15 , Issue. 4 ]

Author(s):

Samar Said Fatahala, Emad Ahmed Shalaby, Shaymaa Emam Kassab and Mossad Said Mohamed   Pages 517 - 526 ( 10 )

Abstract:


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, 1H 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 μg /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.

Keywords:

Anticancer, antioxidant, docking, pyrrole, structure-activity-relationship, synthesis.

Affiliation:

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain- Helwan, Helwan, Cairo. Egypt, Postal code: 1179.

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