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Russ Chem Bull
2013 Jan 01;623:836-843. doi: 10.1007/s11172-013-0113-2.
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Synthesis and antineoplastic properties of (1H-1,2,3-triazol-1-yl)furazans.
Kulikov AS
,
Epishina MA
,
Batog LV
,
Rozhkov VY
,
Makhova NN
,
Konyushkin LD
,
Semenova MN
,
Semenov VV
.
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A method of 3-amino-4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]furazan synthesis was optimized. Condensation of these compounds with 2,5-dimethoxytetrahydrofuran resulted in a series of previously unknown 4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]-3-(pyrrol-1-yl)furazans. All target compounds were evaluated for both antimitotic microtubule destabilizing effect in a phenotypic sea urchin embryo assay and cytotoxicity in a panel of 60 human cancer cell lines. Pyrrolyl derivatives of triazolylfurazans were determined as antiproliferative compounds. The most potent microtubule targeting compounds 7a and 7e are of interest for further trials as antineoplastic agents.
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