Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity

Because of its wide spectrum of targets and biological activities, the oxazole ring is a valuable heterocyclic scaffold in the design of new therapeutic agents with anticancer, antiviral, antibacterial, anti-inflammatory, neuroprotective, antidiabetic and antidepressant properties. The presence of t...

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Autores principales: Marilia Barreca, Virginia Spanò, Maria Valeria Raimondi, Chiara Tarantelli, Filippo Spriano, Francesco Bertoni, Paola Barraja, Alessandra Montalbano
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Lenguaje:EN
Publicado: Elsevier 2021
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Acceso en línea:https://doaj.org/article/19046b374f964d0bb7731ec2a44064d5
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spelling oai:doaj.org-article:19046b374f964d0bb7731ec2a44064d52021-12-03T04:01:36ZRecurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity2772-417410.1016/j.ejmcr.2021.100004https://doaj.org/article/19046b374f964d0bb7731ec2a44064d52021-07-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2772417421000042https://doaj.org/toc/2772-4174Because of its wide spectrum of targets and biological activities, the oxazole ring is a valuable heterocyclic scaffold in the design of new therapeutic agents with anticancer, antiviral, antibacterial, anti-inflammatory, neuroprotective, antidiabetic and antidepressant properties. The presence of two heteroatoms, oxygen and nitrogen, offers possible interactions (hydrogen, hydrophobic, van der Waals or dipoles bonds) with a broad range of receptors and enzymes. Furthermore, the oxazole core conjugates low cytotoxicity with improved compound solubility and is well suited to structural modifications such as substitution with different groups and condensation to aromatic, heteroaromatic or non-aromatic rings, offering diversity when introduced into scaffolds. These features make it a very attractive nucleus in medicinal chemistry.Herein we present a diverse array of oxazole derivatives with potential therapeutic use in multiple tumor models. The emphasis has been addressed to compounds with anti-tubulin activity reported in literature in the last decade, describing their structural features, efficiency and future perspectives.Marilia BarrecaVirginia SpanòMaria Valeria RaimondiChiara TarantelliFilippo SprianoFrancesco BertoniPaola BarrajaAlessandra MontalbanoElsevierarticleOxazolesAnti-Tubulin agentsCancerColchicine binding inhibitorsPharmacy and materia medicaRS1-441Other systems of medicineRZ201-999ENEuropean Journal of Medicinal Chemistry Reports, Vol 1, Iss , Pp 100004- (2021)
institution DOAJ
collection DOAJ
language EN
topic Oxazoles
Anti-Tubulin agents
Cancer
Colchicine binding inhibitors
Pharmacy and materia medica
RS1-441
Other systems of medicine
RZ201-999
spellingShingle Oxazoles
Anti-Tubulin agents
Cancer
Colchicine binding inhibitors
Pharmacy and materia medica
RS1-441
Other systems of medicine
RZ201-999
Marilia Barreca
Virginia Spanò
Maria Valeria Raimondi
Chiara Tarantelli
Filippo Spriano
Francesco Bertoni
Paola Barraja
Alessandra Montalbano
Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
description Because of its wide spectrum of targets and biological activities, the oxazole ring is a valuable heterocyclic scaffold in the design of new therapeutic agents with anticancer, antiviral, antibacterial, anti-inflammatory, neuroprotective, antidiabetic and antidepressant properties. The presence of two heteroatoms, oxygen and nitrogen, offers possible interactions (hydrogen, hydrophobic, van der Waals or dipoles bonds) with a broad range of receptors and enzymes. Furthermore, the oxazole core conjugates low cytotoxicity with improved compound solubility and is well suited to structural modifications such as substitution with different groups and condensation to aromatic, heteroaromatic or non-aromatic rings, offering diversity when introduced into scaffolds. These features make it a very attractive nucleus in medicinal chemistry.Herein we present a diverse array of oxazole derivatives with potential therapeutic use in multiple tumor models. The emphasis has been addressed to compounds with anti-tubulin activity reported in literature in the last decade, describing their structural features, efficiency and future perspectives.
format article
author Marilia Barreca
Virginia Spanò
Maria Valeria Raimondi
Chiara Tarantelli
Filippo Spriano
Francesco Bertoni
Paola Barraja
Alessandra Montalbano
author_facet Marilia Barreca
Virginia Spanò
Maria Valeria Raimondi
Chiara Tarantelli
Filippo Spriano
Francesco Bertoni
Paola Barraja
Alessandra Montalbano
author_sort Marilia Barreca
title Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
title_short Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
title_full Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
title_fullStr Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
title_full_unstemmed Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
title_sort recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
publisher Elsevier
publishDate 2021
url https://doaj.org/article/19046b374f964d0bb7731ec2a44064d5
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