Synthesis and Molecular Docking of New Thiophene Derivatives as Lactate Dehydrogenase-A Inhibitors-Reference-Cited by-同舟云学术

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

Published:2019-05-29 Issue:10 Volume:19 Page:833-841
ISSN:1389-5575
Container-title:Mini-Reviews in Medicinal Chemistry
language:en
Short-container-title:MRMC

Author:

Amr Abd El-Galil E.¹,El-Shehry Mohamed F.²,Ibrahim Alhussein A.³,Hosni Hanaa M.²,Al-Omar Mohamed A.¹,Ghabbour Hazem A.¹

Affiliation:

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

2. Pesticide Chemistry Department, National Research Center, Dokki 12622, Cairo, Egypt

3. Applied Organic Chemistry Department, National Research Centre, 12622, Dokki, Giza, Egypt

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.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmacology,General Medicine

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