Structure-based design and evaluation of synthetic porphyrin derivatives as G-quadruplex stabilizing anticancer agents

R N Bhadane, D B Meshram, R M Gilhotra

Forskningsoutput: TidskriftsbidragArtikelVetenskapligPeer review

Sammanfattning

OBJECTIVE: 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.

OriginalspråkEngelska
Sidor (från-till)103-111
Antal sidor9
TidskriftJournal of Experimental Therapeutics and Oncology
Volym12
Utgåva2
StatusPublicerad - nov 2017
MoE-publikationstypA1 Tidskriftsartikel-refererad

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