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.
Method: 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
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, thieno[2, 3-d]pyrimidin-4(3H)-ones, molecular modeling, lactate dehydrogenase inhibitors,
anticancer drug target, tumor genesis.
Rights & PermissionsPrintExport