1383452-46-7Relevant academic research and scientific papers
Synthesis, characterization and biological evaluation of a novel series of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazines containing an amide linkage
Puthiyapurayil, Pushpan,Poojary, Boja,Buridipad, Sunil Kumar
, p. E55-E67 (2014/10/16)
Two series of combinatorial library of 3,6-disubstituted-7H-1,2,4-triazolo- [3,4-b]-1,3,4-thiadiazines bearing an amide linkage were synthesized. All the newly synthesized compounds were characterized by spectral analyses. The newly synthesized compounds were screened for their cytotoxicity, anti-inflammatory, and analgesic activities. Among the tested compounds, the compound 9g (Ar = 4-(methoxybenzyl)piperazine) is the most promising molecule with half maximal inhibitory concentration (IC50) value of 14.24 μM in (MCF-7) cells. Compounds 9f (Ar = 4-(chlorobenzyl)piperazine), 9g, and 9k (Ar = 2-(fluorophenyl)piperazine) exhibited excellent anti-inflammatory activity at a dose level of 50 mg/kg, almost comparable with the standard drug. In case of analgesic activity among the tested compounds, the compounds 9f, 9g, and 9k showed more potent and consistent activity in both 100 and 200 mg/kg/po doses with less ulcerogenic risk.
Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents
Puthiyapurayil, Pushpan,Poojary, Boja,Chikkanna, Chandrashekhar,Buridipad, Sunil Kumar
, p. 203 - 210 (2012/08/13)
On account of the reported anticancer activity of pyrazoles and oxadiazoles, we have designed and synthesized a novel combinatorial library of S-substituted-1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety and tested for in-vitro cytotoxic activity by MTT assay. Amongst the tested compounds, the compound 5e was the most promising anticancer agent with IC50 value of 15.54 μM in MCF-7 cells, compared to Doxorubicin as standard drug. The newly synthesized compounds were characterized by NOE, IR, 1H NMR, 13C NMR and LC-MS analysis.
