2004
DOI: 10.3390/90300109
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Synthesis and Antitumor Activity of 5-Trifluoromethyl-2,4- dihydropyrazol-3-one Nucleosides

Abstract: 2,4-Dihydropyrazole glucosides 3a-3c were prepared and tested for their antitumor activity. The structures of these compounds were established by 1 H and 13 C-NMR spectroscopy. Glucoside 3b shows an in vitro IC 50 value of 16.4 µM against proliferation of the human promyelotic leukemia (HL60) cell line.

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Cited by 74 publications
(39 citation statements)
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“…The in-vitro anticancer screening of all the prepared compounds was carried out by MTT assay in MCF-7 and BT-549 cell lines. The MTT assay is based on the assumption that living cells reduce tetrazolium due to the presence of mitochondrial SDH, which is absent in the metabolically fluorine substitution in the para regiochemistry 29,30 in the context of the both breast and colon cancers. All compounds other than 5a seem to have moderate cytotoxic activity against mammary carcinoma cell lines.…”
Section: Determination Of Cytotoxicitymentioning
confidence: 99%
“…The in-vitro anticancer screening of all the prepared compounds was carried out by MTT assay in MCF-7 and BT-549 cell lines. The MTT assay is based on the assumption that living cells reduce tetrazolium due to the presence of mitochondrial SDH, which is absent in the metabolically fluorine substitution in the para regiochemistry 29,30 in the context of the both breast and colon cancers. All compounds other than 5a seem to have moderate cytotoxic activity against mammary carcinoma cell lines.…”
Section: Determination Of Cytotoxicitymentioning
confidence: 99%
“…Pyrazolopyrimidines and related fused heterocycles are of interest as potential bioactive molecules. They are known to exhibit pharmacological activities such as CNS-depressant (Abdou et al, 2004;Julino and Stevens, 1998), antiviral (Gadhachanda et al, 2007) anticancer (Capdeville et al, 2002;Taylor et al, 1992;Al-Saadi et al, 2008) and tuberculostatic (Ghorab et al, 2004) activities. Pyrazolo [3,4-d]pyrimidines were identifi ed as a general class of adenosine receptors (Davies et al, 1983(Davies et al, , 1984.…”
Section: Introductionmentioning
confidence: 99%
“…After lot of literature survey we came to know that pyrazolopyrimidines and related fused heterocycles attracted organic chemist very much due to their broad spectrum biological and chemotherapeutic importance. They are known to exhibit widespread pharmacological importance [3][4] and were reported to posses antibacterial [5], antifungal [6], anti-inflammatory [7], antiviral [8], analgesic [9], antitumor [10], CNS-depressant [11][12], neuroleptic [13], tuberculostatic [14], protein kinase inhibitors [15], HIV reverse transcriptase inhibitors [16], non-narcotic analgesic activities [17]. More over pyrazolo [3,4-d]pyrimidines identifies as general class of adenosine receptors [18][19][20].…”
Section: …………………………………………………………………………………………………… Introduction:-mentioning
confidence: 99%