Quadruplex DNA stabilizing agents as potential anti-cancer therapeutics

Medicinal Chemistry

ISSN: 2161-0444

Open Access

Quadruplex DNA stabilizing agents as potential anti-cancer therapeutics

6th World Congress on Medicinal Chemistry and Drug Design

June 07-08, 2017 Milan, Italy

Mrinalkanti Kundu

TCG Lifesciences Pvt. Ltd., India

Posters & Accepted Abstracts: Med Chem (Los Angeles)

Abstract :

Over 100 cancers affect human, as per the World Cancer Report, ~14 million new cases of cancer occurred globally resulting ~15% of deaths in 2012. Towards our goal in improving the quality of life for the people suffering from cancer, we are investigating on the identification of small drug-like compounds as potential G-quadruplex (G4s) binders to treat this disease. DNA integrity is critical for proper cellular function and proliferation and has played a key role as successful molecular target for many of the drugs that have been used for decades. Compounds that target DNA are some of the most effective agents in clinical use and produced increase in cancer patients├ó┬?┬? survival but, they are extremely toxic. Consequently, much effort has been put into finding agents that are more selective and thus presumably will have lesser side effects. Targeting non-canonical DNA secondary structures such as G4s is now considered as an attractive approach toward drug intervention in anti-cancer therapy and thus, significant research is in progress targeting G4 DNAs with small molecules hoping to inhibit cancer growth. We report the design, synthesis of novel small molecules and their evaluation as G4s stabilizing agents. Efficiency of these synthetic compounds was performed to assess the quadruplex binding affinity by using various biophysical and biochemical studies. For the lead compound/s, the binding mode was explained by modeling studies and their in-vitro cell growth inhibition was also tested. Finally, drug-likeness of the selected compounds was evaluated for liver microsomal stability, aqueous solubility, CYP inhibition studies.

Biography :


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