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Structure-based design and evaluation of synthetic porphyrin derivatives as G-quadruplex stabilizing anticancer agents
R. N. Bhadane, D. B. Meshram and R. M. Gilhotra

G-quadruplex structures formed in telomeres and proto-oncogene represent a potentially useful target for anticancer drugs. Stabilization of this arrangement may inhibit the further action of different enzymes involved in cancer cell immortalization. In present work structure-based drug design and synthesis was carried out on series of meso-substituted porphyrin analogues. The interaction of porphyrin derivatives with G-quadruplex DNA has been explored by virtual screening procedure. Some of the potential binding agents were then synthesized and evaluated in-vitro by MTT and PCR stop assay. The study indicates that these compounds had strong G-Quadruplex binding affinity with very good inhibitory activity in MCF-7 and A549 cell lines.

Keywords: G-quadruplex, porphyrin, telomere, protooncogene

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