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SELECTBIO Conferences MedChem India 2017


Boronic acid based Small Molecules as Potential Anticancer Agents

Amit Shard, Assistant Professor, NIPER Ahmedabad

Globally more than 1 million people get colorectal cancer every year resulting in about 715,000 deaths as of 2010 up from 490,000 in 1990. Increased stool (fecal) levels of tumor M2-PK are being investigated as a method of screening for colorectal tumors. Tumor M2-PK is a synonym for the dimeric form of the pyruvate kinase isoenzyme type M2 (PKM2), a key enzyme within tumor metabolism. Tumor M2-PK can be elevated in many tumor types, rather than being an organ-specific tumor marker. The dimeric form of M2-PK has a low affinity for phosphoenolpyruvate, being nearly inactive at physiological PEP concentrations. When M2-PK is mainly in the dimeric form, which is the case in tumor cells, all phosphometabolites above pyruvate kinase accumulate and are channeled into synthetic processes which branch off from glycolytic intermediates, such as nucleic acids, phospholipids and amino acids, important cell building blocks for highly proliferating cells such as tumor cells. Previous attempts to nail this enzyme using various agents have added to library of molecules which have shown in vitro promise but clinical success is far from. Henceforth, there is clearly a pressing need for better treatments for pancreatic cancer.  Here we intend to focus on the design and synthesis of boronic acid based molecules with high affinity towards hard oxygen nucleophiles in comparison to the soft cysteine nucleophiles as per Lewis hard-soft-acid-base principle. The molecules designed are showing excellent interaction with the tumor M2PK in silico and have shown good in vitro activity . The talk will mainly revolve around utilization of similar molecules against tumor M2-PK.

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