Design, synthesis, and in-vitro antiproliferative effect of some novel 1,3,4-oxadiazole derivatives bearing benzimidazole nucleus

Sahoo, Ujjwal; Seth, A. K.; Balaraman, R; Velmurugan, Ramaswamy; Gangawane, Ajit K.

doi:10.4103/1687-4315.172865

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“…A series of 4-{1-[(4-acetyl-5-(substituted)-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl]-5-nitro-1H-benzimidazol-2-yl}benzonitrile and 4-{5-substituted-1-[(4,5-disubstituted)-4,5-dihydro-1,3,4-oxadiazol-2-yl) methyl]-5-nitro-1H-benzimidazol-2-yl} benzonitrile derivatives were synthesized and reported by Sahoo et al (2015). Nine compounds were selected for evaluation of anticancer activity against L929, HCT15, and Hep2 cancer cell lines using MTT assay.…”

Section: 34-oxadiazolesmentioning

confidence: 99%

1,3,4‐oxadiazole and its derivatives: A review on recent progress in anticancer activities

2020

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The 1,3,4-oxadiazole nucleus is a biologically imperative scaffold possesses numerous biological activities. The broad and potent activity of 1,3,4-oxadiazole and their derivatives has established them as important pharmacological scaffolds especially in the treatment of cancer disease. Several di-, tri-, aromatic, and heterocyclic substituted 1,3,4-oxadiazole derivatives have been reported to possess potent anticancer activity. These substituted 1,3,4-oxadiazoles had shown different mechanism of action and participated in anticancer drug discovery and development. This review is complementary to earlier reviews and aims to review the work reported on anticancer activities of 1,3,4-oxadiazole derivatives from year 2000 to the beginning of 2020. K E Y W O R D S 1,3,4-oxadiazole, cancer, histone deacetylase, synthesis, tubulin polymerizations | 573 VAIDYA et Al. anticancer evaluation of 1,3,4-oxadiazole derivatives as inhibitors of Kinesin spindle protein (KSP). KSP inhibitors have been utilized for the treatment of inflammation, hyperplasias, cancer, and immune disorders. Furthermore, Shashikumar and colleagues in year 2015 obtained a WO (World intellectual property organization) patent for 1,3,4-oxadiazoles as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. Theses patented compounds having the ability to boost the immunity and were reported as immunomodulators. The growing patent literature of recent years demonstrates that the 1,3,4-oxadiazoles are becoming of great practical significance. The literature clearly reported numerous mechanism for anticancer activities of substituted 1,3,4-oxadiazole derivatives (Zhang et al., 2010, 2011). Recently, Glomb et al. (2018) published a notable review article, describing antiproliferative effects of 1,3,4-oxadiazoles associated with their numerous mechanisms, including inhibition of growth factors, enzymes, kinases and others. Irrespective of Glomb et al. (2018) review in which they were cited numerous anticancer mechanism of 1,3,4-oxadiazoles, herein we had focused on several 1,3,4-oxadiazole derivatives for their anticancer activity. Especially, we focus this review on in vitro and in vivo anticancer activities of 1,3,4-oxadiazoles in the perspective of cancer drug development and refinement.

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Section: 34-oxadiazolesmentioning

confidence: 99%