Abstract
Synthesis and evaluation of cytotoxicity of a series of heterocyclic compounds derived from 1, 4-bis-(5- [hydrazinocarbonylmethylthio]-4-phenyl-1,2,4-triazol-3-yl) butane (1a-b) are described. The triazolo-triazoles (9-15) and thiadiazoles (16-18) were prepared from respective thiosemicarbazide intermediates (2-8). The Schiff bases (19-24) were prepared from (1a, b) by reacting with different carboxaldehydes in acetic acid medium. All the synthesized compounds were characterized by IR, NMR and Mass spectral studies. The compounds were evaluated for in vitro cytotoxicity potential using the standard MTT assay against a panel of three human cancer cell lines: Lung carcinoma A-549, Colon carcinoma HT-29 and Breast Cancer MDA MB-231. The DNA damage activity of the compound 24 was evaluated by alkaline comet assay.
Keywords: 1, 2, 4-triazoles, 1, 3, 4-thiadiazoles, cytotoxicity, MTT assay, comet assay.
Medicinal Chemistry
Title:Synthesis and in vitro Cytotoxicity Studies of Certain Novel Heterocycles Derived from Bis 1, 2, 4-Triazoles and their DNA Damage Studies
Volume: 9 Issue: 8
Author(s): Madhusudan N. Purohit, Chandrashekhar Venkaraddi Mangannavar and Mayur C. Yergeri
Affiliation:
Keywords: 1, 2, 4-triazoles, 1, 3, 4-thiadiazoles, cytotoxicity, MTT assay, comet assay.
Abstract: Synthesis and evaluation of cytotoxicity of a series of heterocyclic compounds derived from 1, 4-bis-(5- [hydrazinocarbonylmethylthio]-4-phenyl-1,2,4-triazol-3-yl) butane (1a-b) are described. The triazolo-triazoles (9-15) and thiadiazoles (16-18) were prepared from respective thiosemicarbazide intermediates (2-8). The Schiff bases (19-24) were prepared from (1a, b) by reacting with different carboxaldehydes in acetic acid medium. All the synthesized compounds were characterized by IR, NMR and Mass spectral studies. The compounds were evaluated for in vitro cytotoxicity potential using the standard MTT assay against a panel of three human cancer cell lines: Lung carcinoma A-549, Colon carcinoma HT-29 and Breast Cancer MDA MB-231. The DNA damage activity of the compound 24 was evaluated by alkaline comet assay.
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Purohit N. Madhusudan, Mangannavar Venkaraddi Chandrashekhar and Yergeri C. Mayur, Synthesis and in vitro Cytotoxicity Studies of Certain Novel Heterocycles Derived from Bis 1, 2, 4-Triazoles and their DNA Damage Studies, Medicinal Chemistry 2013; 9 (8) . https://dx.doi.org/10.2174/1573406411309080008
DOI https://dx.doi.org/10.2174/1573406411309080008 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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