Synthesis, β-glucuronidase inhibition and molecular docking studies of cyano-substituted bisindole hydrazone hybrids.


Journal

Molecular diversity
ISSN: 1573-501X
Titre abrégé: Mol Divers
Pays: Netherlands
ID NLM: 9516534

Informations de publication

Date de publication:
May 2021
Historique:
received: 29 01 2020
accepted: 03 04 2020
pubmed: 18 4 2020
medline: 23 11 2021
entrez: 18 4 2020
Statut: ppublish

Résumé

The β-glucuronidase, a lysosomal enzyme, catalyzes the cleavage of glucuronosyl-O-bonds. Its inhibitors play a significant role in different medicinal therapies as they cause a decrease in carcinogen-induced colonic tumors by reducing the level of toxic substances present in the intestine. Among those inhibitors, bisindole derivatives had displayed promising β-glucuronidase inhibition activity. In the current study, hydrazone derivatives of bisindolymethane (1-30) were synthesized and evaluated for in vitro β-glucuronidase inhibitory activity. Twenty-eight analogs demonstrated better activity (IC

Identifiants

pubmed: 32301032
doi: 10.1007/s11030-020-10084-4
pii: 10.1007/s11030-020-10084-4
doi:

Substances chimiques

Glycoproteins 0
Hydrazones 0
Indoles 0
beta-glucuronidase inhibitor 0
Glucuronidase EC 3.2.1.31

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

995-1009

Subventions

Organisme : Kementerian Pendidikan Malaysia
ID : 600-IRMI/FRGS 5/3 (111/2019)
Organisme : Kementerian Pendidikan Malaysia
ID : 600-RMI/FRGS 5/3 (0065/2016)
Organisme : Universiti Teknologi MARA (MY)
ID : 600-IRMI/PERDANA 5/3 BESTARI (041/2018)

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Auteurs

Obaidurahman Abid (O)

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia.
Faculty of Applied Science, Universiti Teknologi MARA (UiTM), 40450, Shah Alam, Selangor, Malaysia.
Department of Chemistry, Faculty of Science, Nangarhar University, Jalalabad, Nangarhar, 2601, Afghanistan.

Syahrul Imran (S)

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia. imran@isiswa.uitm.edu.my.
Faculty of Applied Science, Universiti Teknologi MARA (UiTM), 40450, Shah Alam, Selangor, Malaysia. imran@isiswa.uitm.edu.my.

Muhammad Taha (M)

Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Saudi Arabia. taha_hej@yahoo.com.

Nor Hadiani Ismail (NH)

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia.
Faculty of Applied Science, Universiti Teknologi MARA (UiTM), 40450, Shah Alam, Selangor, Malaysia.

Waqas Jamil (W)

Institute of Advanced Research Studies in Chemical Sciences, University of Sindh Jamshoro, Hyderabad, 76080, Pakistan.

Syed Muhammad Kashif (SM)

Institute of Advanced Research Studies in Chemical Sciences, University of Sindh Jamshoro, Hyderabad, 76080, Pakistan.

Khalid Mohammed Khan (KM)

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.

Juliana Yusoff (J)

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia.

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Classifications MeSH