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

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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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



Anti-Cancer Agents in Medicinal Chemistry, 15(4): 517-526.

Author(s): Samar Said Fatahala, Emad Ahmed Shalaby, Shaymaa Emam Kassab and Mossad Said Mohamed.

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

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.



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Article Details

Volume: 15
Issue Number: 4
First Page: 517
Last Page: 526
Page Count: 10
DOI: 10.2174/1871520615666150105113946
Price: $58
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