6726-49-4Relevant academic research and scientific papers
Structural studies on bioactive compounds. 1 Heck reactions on 4-methylenepyrazolo[5,1-c][1,2,4]triazines
Iwashita, Eiichiro,Williams, Huw E. L.,Hutchinson, Ian,Stevens, Malcolm F. G.
experimental part, p. 115 - 120 (2009/08/15)
1-(3-Methyl-4-methylenepyrazolo[5,1-c][1,2,4]triazin-6(4H-yl)ethanone 9a and its 7-methyl- 9b and 7-phenylderivative 9c undergo Heck coupling to afford (Z)-1-{4-benzylidene-3-methylpyrazolo[5,1-c][1,2,4]triazin-6(4H)- yl}ethanones 10a-c and substituted benzylidene analogues 10d-m as the major geometrical isomers in low yields. The most potent agent in a human tumour screen in vitro was 10b (mean GI50 value 4.9 mM in a panel of 60 human cancer cell lines), with evidence of selective action against colon KM12 (GI50 0.02 mM) and breast MCF-7 tumour cell lines (GI501.35 mM).
