Synthesis and screening of some novel substituted indoles contained 1,3,4-oxadiazole and 1,2,4-triazole moiety

Gadegoni, Hemalatha; Sarangapani, M.

doi:10.1016/j.cclet.2013.01.001

Cited by 30 publications

(17 citation statements)

References 23 publications

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“…Schiff bases are very accomplished ligands in transition metal as well as inner‐transition metal complexes with suitable properties for theoretical and practical applications . Heterocyclic Schiff bases derived from 1,2,4‐triazoles have received much attention, particularly in the study of complex formation because they exhibit interesting biological activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, structural characterization and biological studies of neodymium(III) and samarium(III) complexes with mercaptotriazole Schiff bases

Ain

Pandey

et al. 2015

Applied Organom Chemis

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A series of neodymium(III) and samarium(III) complexes of type [Ln(L)Cl(H 2 O) 3 ] have been synthesized with Schiff bases (LH 2 ) derived from 3-(phenyl/substituted phenyl)-4-amino-5-mercapto-1,2,4-triazoles and isatin. The structures of the complexes were established using elemental analysis, molar conductivities, magnetic moments, infrared, NMR ( 1 H, 13 C) and UV-visible spectra, X-ray diffraction and mass spectrometry. The thermal behaviour of these compounds under non-isothermal conditions was investigated using thermogravimetry and differential thermogravimetry. The intermediates obtained at the end of various thermal decomposition steps were identified from elemental analysis and infrared spectral studies. All the ligands and their complexes were also screened for their antibacterial activity against Staphylococcus aureus and Bacillus subtilis and antifungal activity against Aspergillus niger, Aspergillus flavus and Colletotrichum capsici. The screening results were correlated with the structural features of the compounds.

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Section: Introductionmentioning

confidence: 99%

Synthesis, structural characterization and biological studies of neodymium(III) and samarium(III) complexes with mercaptotriazole Schiff bases

Ain

Pandey

et al. 2015

Applied Organom Chemis

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“…1,3,4-Oxadiazoles are an important class of heterocyclic compounds with a wide range of biological activities. [4][5][6] Among these, a few different substituted 1,3,4-oxadiazoles have exhibited potent antitumor activities. [7][8][9][10] Recently, a series of new 1,3,4-oxadiazole derivatives incorporating a pyridine moiety were synthesized and developed as potential telomerase inhibitors.…”

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confidence: 99%

Synthesis and Anticancer Evaluation of 1,3,4-Oxadiazoles, 1,3,4-Thiadiazoles, 1,2,4-Triazoles and Mannich Bases

Abdo

Kamel

2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydrazide. Aminoalkylation of compounds 5a-d with formaldehyde and various secondary amines furnished the Mannich bases 6a-p. The structures of the newly synthesized compounds were confirmed on the basis of their spectral data and elemental analyses. All the compounds were screened for their in vitro anticancer activity against six human cancer cell lines and normal fibroblast cells. Sixteen of the tested compounds exhibited significant cytotoxicity against most cell lines. Among these derivatives, the Mannich bases 6j, 6m and 6p were found to exhibit the most potent activity. The Mannich base 6m showed more potent cytotoxic activity against gastric cancer NUGC (IC50=0.021 µM) than the standard CHS 828 (IC50=0.025 µM). Normal fibroblast cells WI38 were affected to a much lesser extent (IC50>10 µM).

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“…To overcome the MDR limitations many research has taken place and in that oxadiazole is one of the promising scaffold in the medicinal chemistry [2]. Oxadiazoles are physiologically active heterocyclic compounds owing to a vast sphere of biological activities, including anticancer [3][4][5][6][7][8][9][10][11], antidiabetic [12], antiviral [13,14], anti-inflammatory [15,16], antibacterial [17,18], antifungal [19], antimycobacterial [20], analgesic [21], anticonvulsant [22], tyrokinase inhibitor [23] and cathepsin K inhibitor [24] antioxidant [25] properties.…”

Section: Introduction and Experimentalmentioning

confidence: 99%

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

2020

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A unique series oxadiazoles were synthesized by cyclization of benzophenone hydrazide, followed by the nucleophillic alkylation of heterocyclic scaffold. Synthesized title compounds were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for the anticancer activity. IC 50 values of the 7h observed for in-vitro anti-cancer activities were 112.6 µg/ml and 126.7 µg/ml, against the MCF-7 and KB cell lines respectively. Most active compounds were found to be less toxic, which were determined by MTT assay method with normal cell line (L292). Biological screening of the synthesized series of compounds reveals that, Compound 7h was the potent molecule.Electronic supplementary material The online version of this article (https ://doi.org/10.1007/s4245 2-020-2511-z) contains supplementary material, which is available to authorized users. * S. V. Mamatha, mamatha.zh32@yahoo.com |

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Synthesis and screening of some novel substituted indoles contained 1,3,4-oxadiazole and 1,2,4-triazole moiety

Cited by 30 publications

References 23 publications

Synthesis, structural characterization and biological studies of neodymium(III) and samarium(III) complexes with mercaptotriazole Schiff bases

Synthesis, structural characterization and biological studies of neodymium(III) and samarium(III) complexes with mercaptotriazole Schiff bases

Synthesis and Anticancer Evaluation of 1,3,4-Oxadiazoles, 1,3,4-Thiadiazoles, 1,2,4-Triazoles and Mannich Bases

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

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