N-substituted pyrrole-based scaffolds as potential anticancer and antiviral lead structures
2015
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 (IC 50 :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 (EC 50 : 27-40 µM).
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