N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures

作者：Pegklidou Kyriaki; Papastavrou Nikolaos; Gkizis Petros; Komiotis Dimitrios; Balzarini Jan; Nicolaou Ioannis^*

来源：Medicinal Chemistry, 2015, 11(6): 602-608.

DOI：10.2174/1573406411666150313161225

• N-substituted pyrroles
• antiproliferative agents
• antiviral activity

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 pyrrole-based 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 mu M) 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 mu M).

• 出版日期2015
• 单位河北医科大学