Investigation of the Cytotoxic Potencies of substituted dipyrrolo[1,2-a:2',1'-c]pyrazines and substituted pyrrolo[2'',1'':3',4']pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-8(9H)-ones

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Document Type : Original Article

Authors

1 Faculty of Chemistry, Semnan University, Semnan, Iran

2 Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medica

Abstract

Cancer is the world's second leading cause of death after cardiovascular diseases. The data reported by the World Health Organization (WHO) about this disease indicates a troubling increase in both prevalence and mortality over the past decade. Consequently, significant efforts have been directed toward the discovery and development of a new and potent anticancer agents. In an attempt to find and develop further new compounds possessing cytotoxic potencies, the efficient, simple, and multi-step synthetic routes were employed to afford various substituted dihydrodipyrrolo[1,2-a:2',1'-c]pyrazine-2,3-dicarboxylates 8a-8s, which were subsequently subjected to cyclization in the presence of hydrazine hydrate to produce tetrahydropyrrolo[2'',1'':3',4']pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-8(9H)-ones 10a-10q. Afterwards, their cytotoxicity were examined against five human cancerous cell lines, including MCF7, HeLa, SW480, HepG2, and A549 by using the MTT colorimetric assay. Considering the results, further evaluations were conducted on the compound 8l, which exhibited the induction of apoptosis and G0 cell cycle arrest in MCF7 and A549 cells.

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Applied Chemistry Today

Articles in Press, Accepted Manuscript
Available Online from 18 June 2024

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