Synthesis, characterization and cytotoxic evaluation of novel derivatives of 1, 3, 4-oxadiazole containing 5-phenyl thiophene moiety

Adimule, Vinayak; Sudha, Medapa; Jagadeesha, AdarshaHaraballi; Kumar, LalitaSanjeev; Rao, Prakash Kumar

doi:10.9790/3008-09544248

Cited by 10 publications

(5 citation statements)

References 12 publications

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“…Schiff base compounds of various halogens substituted aromatic carbohydrazides with 5-phenylthiophene moiety, on cyclizing with chloramine-T as promoter improves the total polar surface area and increases the water solubility. Thus, Adimule et al (2014) combined the 5-phenyl thiophene with different halogen substituted aromatic carbohydrazides to obtain new derivatives of 1,3,4-oxadiazoles. A series of novel derivatives of 1,3,4-oxadiazoles containing 5-phenyl thiophene moiety had been synthesized by cyclizing schiff base derivatives with chloramine-T. All the synthesized compounds were characterized by spectral analyses, and studied for their anticancer activities against Caco-2, HepG2 and PANC-1 cancer cell lines.…”

Section: Oxadiazole Derivativesmentioning

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: Oxadiazole Derivativesmentioning

confidence: 99%

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

2020

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“…7 It serves as a bioisostere for carbonyl-containing compounds like esters, amides, and carbamates in certain instances, while also serving as a planar aromatic linker to achieve the desired molecular geometry. 8 The derivatives of oxadiazoles play a very significant role in medicinal chemistry as they have the properties like analgesic, 9 anticancer, 10 antiproliferative, 11 cytotoxic, 12 sedative, 13 etc., 1,3,4-oxadiazoles are commonly prepared through the utilization of carbohydrazides, Schiff bases, and diacylhydrazines. Numerous oxidizing agents and cyclizing agents can be employed for their synthesis, such as those that are readily accessible, namely, phosphorus oxy chloride, 14 iodobenzene diacetate, 15 and FeCl 3 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Molecular Docking, and Anticonvulsant Activity of 1,3,4-Oxadiazole Derivatives

Balachandra,

Deshpande,

Raj

et al. 2024

Journal of Health and Allied Sciences NU

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A novel series of 1,3,4-oxadiazoles (O1–4) were synthesized and physical characterization was done by spectroscopic data (infrared, mass, proton nuclear magnetic resonance). To ascertain the synthesized compound's likely binding mechanism and affinity toward the protein target (Protein Data Bank ID: 3R7X), molecular docking was performed. The synthesized compounds were subjected to in silico analysis using Schrodinger suite 2020–4 and absorption, distribution, metabolism, and excretion screening. Some of the synthesized compounds were subjected to in vivo evaluation of anticonvulsant activity by maximal electroshock seizure and pentylenetetrazol model. The synthesized 1,3,4-oxadiazole analogs may be developed as lead compounds and effective anticonvulsant agents for the pharmaceutical industry based on computational and in vivo data.

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“…[10][11][12][13].In medicine, they enable targeted drug delivery and precise imaging, enhancing treatments while reducing side effects. Electronics benefit from their size, enhancing device performance and enabling flexible displays [14][15][16][17][18][19]. Moreover, in environmental science, nonmaterial plays a role in pollution remediation.…”

Section: Introductionmentioning

confidence: 99%

Low Temperature Chemical Synthesis and Investigation of Cadmium Substituted of Structural Properties of Cobalt Nano Ferrites

Kashid,

Mathad,

Shedam

et al. 2024

JMNM

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This article presents, the systematic and successful preparation of cadmium substituted cobalt ferrite (Co1-xCdxFe2O4) nanoparticles via simple co-precipitation method. X-ray diffraction study confirmed the prepared ferrite nanoparticles were crystallized with a mono phase cubic spinel structure of Fd3m space group. The average crystallite size (Dxrd) was increased with Cd doping content, due to the replacement of Co2+ ions by Cd2+ ions. XRD pattern revealed the high intense peak corresponds to (311) lattice plane and confirmed the formation of cubic structure ferrite nanoparticles. Morphological study was done by using SEM images. The grain size found to be increased with Cd concentration and it reaches the highest of around 0.9μm for Co0.52Cd0.48Fe2O4 composition. Fourier Transform Infrared spectroscopy of prepared samples was recorded in the range of 1000-350 cm-1, confirmed the spinel structure.

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Synthesis, characterization and cytotoxic evaluation of novel derivatives of 1, 3, 4-oxadiazole containing 5-phenyl thiophene moiety

Abstract: Abstract:In the present work a series of novel derivatives of 1,3,4-

Cited by 10 publications

References 12 publications

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

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

Synthesis, Molecular Docking, and Anticonvulsant Activity of 1,3,4-Oxadiazole Derivatives

Low Temperature Chemical Synthesis and Investigation of Cadmium Substituted of Structural Properties of Cobalt Nano Ferrites

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