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Synthesis and Molecular Docking of New Thiophene Derivatives as Lactate Dehydrogenase-A Inhibitors

Abd El-Galil E Amr^1,2, Mohamed F El-Shehry³, Alhussein A Ibrahim²

¹Drug Exploration & Development Chair (DEDC), Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Mini Reviews in Medicinal Chemistry

|February 15, 2019

Abstract

Background & Objective:

A series of novel derivatives possessing the thiophene moiety were synthesized using ethyl 5'-amino-2,3'-bithiophene-4'-carboxylate as the starting material.

Methods:

The new synthesized derivatives were screened as lactate dehydrogenase (LDH) inhibitors. LDH plays an important role in glucose metabolism in cancer cells and can affect tumor genesis and metastasis.

Results:

3-Substituted p-tolylthieno[2,3-d]pyrimidin-4(3H)-ones 4 were the most potent inhibitors in this study compared to Galloflavin reference drug.

Conclusion:

Molecular docking studies on the Human Lactate Dehydrogenase active site were carried out on the synthesized compounds and the MolDock scores ranged between -127 to -171.

Keywords:

Thiophene derivatives anticancer drug target lactate dehydrogenase inhibitors molecular modeling thieno[2,3-d]pyrimidin-4(3H)-ones tumor genesis.

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