Abstract
Undoubtedly, efficient cancer treatment has been a significant challenge for the scientific community over the last decades. Despite tremendous progress made towards this direction, there are still efforts needed to discover new anticancer drugs. In this work, a series of N-substituted pyrrolebased scaffolds have been synthesized and evaluated for antiproliferative activity against a panel of cancer cell lines (L1210, CEM and HeLa). Furthermore, in order to discover new scaffolds as antiviral agents, all the examined compounds were evaluated for activity against different types of DNA and RNA viruses. The key feature of the above structures is the existence of an aromatic ring with at least one hydrogen-bonding donor and acceptor group. Results have shown noteworthy cytostatic activity for three of the synthesized compounds (1, 3 and 9). Especially, compound 1, containing a tropolone ring, proved to be the most promising scaffold (IC50:10-14 µM ) for the development of novel potential anticancer agents. In addition, compound 1 has shown modest anti-HSV-1, -HSV2 activity in HEL cell cultures (EC50: 27-40 µM).
Keywords: N-substituted pyrroles, antiproliferative agents, antiviral activity.
Medicinal Chemistry
Title:N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures
Volume: 11 Issue: 6
Author(s): Kyriaki Pegklidou, Nikolaos Papastavrou, Petros Gkizis, Dimitrios Komiotis, Jan Balzarini and Ioannis Nicolaou
Affiliation:
Keywords: N-substituted pyrroles, antiproliferative agents, antiviral activity.
Abstract: Undoubtedly, efficient cancer treatment has been a significant challenge for the scientific community over the last decades. Despite tremendous progress made towards this direction, there are still efforts needed to discover new anticancer drugs. In this work, a series of N-substituted pyrrolebased scaffolds have been synthesized and evaluated for antiproliferative activity against a panel of cancer cell lines (L1210, CEM and HeLa). Furthermore, in order to discover new scaffolds as antiviral agents, all the examined compounds were evaluated for activity against different types of DNA and RNA viruses. The key feature of the above structures is the existence of an aromatic ring with at least one hydrogen-bonding donor and acceptor group. Results have shown noteworthy cytostatic activity for three of the synthesized compounds (1, 3 and 9). Especially, compound 1, containing a tropolone ring, proved to be the most promising scaffold (IC50:10-14 µM ) for the development of novel potential anticancer agents. In addition, compound 1 has shown modest anti-HSV-1, -HSV2 activity in HEL cell cultures (EC50: 27-40 µM).
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Pegklidou Kyriaki, Papastavrou Nikolaos, Gkizis Petros, Komiotis Dimitrios, Balzarini Jan and Nicolaou Ioannis, N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures, Medicinal Chemistry 2015; 11 (6) . https://dx.doi.org/10.2174/1573406411666150313161225
DOI https://dx.doi.org/10.2174/1573406411666150313161225 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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