Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A

Abdul Malek S. Sherif A.; Ahmed M. Alafeefy; Agnese Balode; Igor Vozny; Aleksandrs Pustenko; Mohey Eldin El Shikh; Fatmah A.S. Alasmary; Abdel Malek Sherif A.; Raivis Žalubovskis

doi:10.1080/14756366.2017.1404593

Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A

Abdul Malek S. Sherif A.
, Ahmed M. Alafeefy
, Agnese Balode
, Igor Vozny
, Aleksandrs Pustenko
, Mohey Eldin El Shikh
, Fatmah A.S. Alasmary
, Abdel Malek Sherif A.
, Raivis Žalubovskis

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC₅₀ = 117–174 µM. Seven compounds exhibited better LDHA inhibition (IC₅₀ 117–136 µM) compared to known LDH inhibitor–galloflavin (IC₅₀ 157 µM).

Original language	English
Pages (from-to)	147-150
Number of pages	4
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume	33
Issue number	1
DOIs	https://doi.org/10.1080/14756366.2017.1404593
State	Published - 1 Jan 2018
Externally published	Yes

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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

inhibitors
Lactate dehydrogenase
triazole

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10.1080/14756366.2017.1404593

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Sherif A., A. M. S., Alafeefy, A. M., Balode, A., Vozny, I., Pustenko, A., El Shikh, M. E., Alasmary, F. A. S., Sherif A., A. M., & Žalubovskis, R. (2018). Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A. Journal of Enzyme Inhibition and Medicinal Chemistry, 33(1), 147-150. https://doi.org/10.1080/14756366.2017.1404593

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title = "Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A",

abstract = "A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117–174 µM. Seven compounds exhibited better LDHA inhibition (IC50 117–136 µM) compared to known LDH inhibitor–galloflavin (IC50 157 µM).",

keywords = "inhibitors, Lactate dehydrogenase, triazole",

author = "\{Sherif A.\}, \{Abdul Malek S.\} and Alafeefy, \{Ahmed M.\} and Agnese Balode and Igor Vozny and Aleksandrs Pustenko and \{El Shikh\}, \{Mohey Eldin\} and Alasmary, \{Fatmah A.S.\} and \{Sherif A.\}, \{Abdel Malek\} and Raivis {\v Z}alubovskis",

note = "Publisher Copyright: {\textcopyright} 2017 The Author(s). Published by Informa UK Limited, trading as Taylor \& Francis Group.",

year = "2018",

month = jan,

day = "1",

doi = "10.1080/14756366.2017.1404593",

language = "English",

volume = "33",

pages = "147--150",

journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",

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}

Sherif A., AMS, Alafeefy, AM, Balode, A, Vozny, I, Pustenko, A, El Shikh, ME, Alasmary, FAS, Sherif A., AM & Žalubovskis, R 2018, 'Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A', Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 33, no. 1, pp. 147-150. https://doi.org/10.1080/14756366.2017.1404593

TY - JOUR

T1 - Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A

AU - Sherif A., Abdul Malek S.

AU - Alafeefy, Ahmed M.

AU - Balode, Agnese

AU - Vozny, Igor

AU - Pustenko, Aleksandrs

AU - El Shikh, Mohey Eldin

AU - Alasmary, Fatmah A.S.

AU - Sherif A., Abdel Malek

AU - Žalubovskis, Raivis

PY - 2018/1/1

Y1 - 2018/1/1

N2 - A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117–174 µM. Seven compounds exhibited better LDHA inhibition (IC50 117–136 µM) compared to known LDH inhibitor–galloflavin (IC50 157 µM).

AB - A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117–174 µM. Seven compounds exhibited better LDHA inhibition (IC50 117–136 µM) compared to known LDH inhibitor–galloflavin (IC50 157 µM).

KW - inhibitors

KW - Lactate dehydrogenase

KW - triazole

UR - https://www.scopus.com/pages/publications/85038351577

U2 - 10.1080/14756366.2017.1404593

DO - 10.1080/14756366.2017.1404593

M3 - Article

C2 - 29199484

AN - SCOPUS:85038351577

SN - 1475-6366

VL - 33

SP - 147

EP - 150

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

IS - 1

ER -

Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A

Abstract

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Keywords

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