1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents

Five member heterocyclic 1,3,4-oxadiazole nucleus find unique place in medicinal chemistry and plays significant role in producing anticancer activity. The small and simple 1,3,4-oxadiazole nucleus is present in various compounds involved in research aimed at evaluating new products that posses inte...

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Veröffentlicht in:European journal of medicinal chemistry 2015-06, Vol.97, p.124-141
Hauptverfasser: Bajaj, Shalini, Asati, Vivek, Singh, Jagadish, Roy, Partha Pratim
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Sprache:eng
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Zusammenfassung:Five member heterocyclic 1,3,4-oxadiazole nucleus find unique place in medicinal chemistry and plays significant role in producing anticancer activity. The small and simple 1,3,4-oxadiazole nucleus is present in various compounds involved in research aimed at evaluating new products that posses interesting pharmacological properties such as antitumour activity. Mono and 2,5-di-substituted-1,3,4-oxadiazole derivatives have attracted considerable attention owing to their effective biological activity and extensive use. The important mechanism involved during its tumour suppression is related with the inhibition of different growth factors, enzymes and kinases including telomerase enzyme, histone deacetylase (HDAC), methionine aminopeptidase (MetAP), thymidylate synthase (TS), glycogen synthase kinase-3 (GSK), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF) and focal adhesion kinase (FAK). The focused criteria of this review is to highlights the targeted inhibitory activity of 1,3,4-oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents. 1,3,4-oxadizole derivatives targated on growth factors, enzymes and kinases has been described to improve anticancer properties. [Display omitted] •Anti-cancer activity of 1,3,4-oxadizole derivatives.•Telomerase enzyme inhibitors and their SARs.•VEGF inhibitors and their SARs.•EGF inhibitors and their SARs.•Glycogen synthase kinase-3b inhibitors and their SARs.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2015.04.051