Imidazo[2,1-b]thiazole based indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor: Structure based design, synthesis, bio-evaluation and docking studies.

Humans Structure-Activity Relationship Enzyme Inhibitors / chemistry HEK293 Cells Indoleamine-Pyrrole 2,3,-Dioxygenase Protein Binding
3-dioxygenase IDO1 inhibitor Imidazo[2,1-b]thiazole Imidazole Indoleamine-2 l-tryptophan

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
15 11 2023
Historique:
received: 27 06 2023
revised: 25 09 2023
accepted: 18 10 2023
medline: 20 11 2023
pubmed: 23 10 2023
entrez: 22 10 2023
Statut: ppublish

Résumé

Indoleamine-2,3-dioxygenase 1 (IDO1) is an immunomodulatory enzyme known to catalyse the initial and rate limiting step of kynurenine pathway of l-tryptophan metabolism. IDO1 enzyme over expression plays a crucial role in progression of cancer, malaria, multiple sclerosis and other life-threatening diseases. Several efforts over the last two decades have been invested by the researchers for the discovery of different IDO1 inhibitors and the plasticity of the IDO1 enzyme ligand binding pocket provide ample opportunities to develop new heterocyclic scaffolds targeting this enzyme. In the present work, based on the X-ray crystal structure of human IDO1 coordinated with few ligands, we designed and synthesized new fused heterocyclic compounds and evaluated their potential human IDO1 inhibitory activity (compound 30 and 41 showed IC

Identifiants

DOI: 10.1016/j.bmcl.2023.129532 PMID: 37866714
pubmed: 37866714
pii: S0960-894X(23)00410-9
doi: 10.1016/j.bmcl.2023.129532
pii:
doi:

Substances chimiques

Enzyme Inhibitors 0
Indoleamine-Pyrrole 2,3,-Dioxygenase 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

129532

Informations de copyright

Copyright © 2023 Elsevier Ltd. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Rahul Singh (R)

Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

Ravinder Kumar (R)

Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

Ashalata Roy (A)

Department of Chemistry, Indian Institute of Technology, Guwahati 781039, India.

Pabitra Mohan Behera (PM)

Institute of Life Science, Nalco Square, Chandrasekharpur, Bhubaneswar 751023, India.

Ankit K Atri (AK)

Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

Kushvinder Kumar (K)

Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.

Debasis Manna (D)

Department of Chemistry, Indian Institute of Technology, Guwahati 781039, India.

Anshuman Dixit (A)

Institute of Life Science, Nalco Square, Chandrasekharpur, Bhubaneswar 751023, India.

Madhuri T Patil (MT)

Department of Chemistry, Mehr Chand Mahajan DAV College for Women, Chandigarh 160 036, India.

R Mankamna Kumari (R)

Department of Biotechnology, School of Life Sciences, Central University of Rajasthan, Ajmer 305 801, India.

Surendra Nimesh (S)

Department of Biotechnology, School of Life Sciences, Central University of Rajasthan, Ajmer 305 801, India.

Deepak B Salunke (DB)

Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India; National Interdisciplinary Centre of Vaccine, Immunotherapeutics and Antimicrobials, Panjab University, Chandigarh 160014, India. Electronic address: salunke@pu.ac.in.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Imidazo[2,1-b]thiazole based...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Imidazo[2,1-b]thiazole based...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Imidazo[2,1-b]thiazole based...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HEK293 › Imidazo[2,1-b]thiazole based...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxygénases › Dioxygenases › Indoleamine-pyrrole 2,3,-dioxygenase › Imidazo[2,1-b]thiazole based...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Imidazo[2,1-b]thiazole based...