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

Reference34 articles.

1. Äikiä M, Jutila L, Salmenperä T, Mervaala E, Kälviäinen R. Long-term effects of tiagabine monotherapy on cognition and mood in adult patients with chronic partial epilepsy.

2. Almsherqi ZA, McLachlan CS, Mossop P, Deng Y. Optimal antiplatelet treatment for percutaneous coronary intervention: Clopidogrel ticlopidine.

3. Hunziker ME, Suehs BT, Bettinger TL, Crismon L. Duloxetine hydrochloride: A new dual-acting medication for the treatment of major depressive disorder.

4. Waugh CD. Tioconazole, In xPharm: The Comprehensive PharmacologyReference, edited by S.J. Enna and David B. Bylund, Elsevier,New York.

5. Cuyun LO, Kaneko M, Takafuta T, Satoh K, Ohnishi M, Yatomi Y, Ozaki Y. Inhibitory effects of ticlopidine on platelet function as assessed by three different methods.

Cited by 2 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Tailored upconversion nanomaterial: A hybrid nano fluorescent sensor for evaluating efficacy of lactate dehydrogenase inhibitors as anticancer drugs;Sensors and Actuators B: Chemical;2021-10

2. Chiral Pyridine-3,5-bis- (L-phenylalaninyl-L-leucinyl) Schiff Base Peptides as Potential Anticancer Agents: Design, Synthesis, and Molecular Docking Studies Targeting Lactate Dehydrogenase-A;Molecules;2020-02-29