Discovery of Novel N-Acylhydrazone Derivatives as Potent Inhibitors of Sirtuin-1

to related objects

SIRT1 enzyme is a key family member of Silent Information Regulators (Sirtuins), which catalyze the deacetylation of proteins. Therefore, developing new SIRT1 inhibitors has potential application in treating cancer disease and age-related metabolic disorders. In this study, we synthesized a series of N-acylhydrazone (NAH) derivatives and performed high-throughput screening of their inhibitory activity against the recombinant SIRT1 protein by a luminescent assay. Using in silico screening, we identified a new NAH derivative that features both selectivity and a high binding affinity towards the active pocket of SIRT1 that are comparable to known inhibitors such as Ex527 and Sirtinol. Such high binding affinity makes the new derivatives promising alternatives to the available inhibitors and holds promise for developing better-targeted drugs against SIRT1 activity.

Location: Deutsche Nationalbibliothek Frankfurt am Main

Extent: Online-Ressource

Language: Englisch

Bibliographic citation: Discovery of Novel N-Acylhydrazone Derivatives as Potent Inhibitors of Sirtuin-1 ; volume:08 ; number:02 ; year:2024 ; pages:100-108
SynOpen ; 08, Heft 02 (2024), 100-108

Contributor: Lipson, Victoria V.
Yaremenko, Fedyr G.
Vakula, Volodymyr M.
Kovalenko, Svitlana V.
Kyrychenko, Alexander V.
Desenko, Sergiy M.
Borysko, Petro О.
Zozulya, Sergiy O.

DOI: 10.1055/s-0043-1763747

URN: urn:nbn:de:101:1-2405231007405.351577714456

Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.

Last update: 14.08.2025, 11:00 AM CEST

Data provider

This object is provided by:
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.

Show original at data provider

Associated

Lipson, Victoria V.
Yaremenko, Fedyr G.
Vakula, Volodymyr M.
Kovalenko, Svitlana V.
Kyrychenko, Alexander V.
Desenko, Sergiy M.
Borysko, Petro О.
Zozulya, Sergiy O.

Other Objects (12)

Hochschulschrift

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Hochschulschrift

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Hochschulschrift

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Cultural heritage institutions wishing to register will find more information here.

Fields marked * need to be filled in.

Username*

Please enter your username

Email*

Please enter your email address

Please do not fill this field

First name

Last name

Password*

Please enter your password

Confirm password*

Please enter the same password

I have read the terms of use and the privacy policy for the collection of personal data and accept them. *

This field is required.

I would like to subscribe to the newsletter of the Deutsche Digitale Bibliothek. See newsletter subscription info.

Account created

Your "My DDB" account has been successfully created. Before you can log in to your account, you must click the confirmation link in the message we just sent to the email address you provided.

Discovery of Novel N-Acylhydrazone Derivatives as Potent Inhibitors of Sirtuin-1

Object Details

References and Relationships

Contributors, Places and Time

Further information

Data provider

Associated

Other Objects (12)

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Identifikation neuer Sirtuin Inhibitoren und Aktivatoren

Discovery of Novel Soluble Epoxide Hydrolase Inhibitors as Potent Vasodilators

Data-driven discovery of potent small molecule ice recrystallisation inhibitors

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Theoretical investigation and design of some indole derivatives as potent β-glucuronidase inhibitors

Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors

Discovery of potent inhibitors of α-synuclein aggregation using structure-based iterative learning

Related objects

Reset password