A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91% and 41% of the tested cell lines, resp.
DIANA P, CARBONE A, BARRAJA P, MARTORANA A, GIA O, DALLAVIA L, et al. (2007). 3,5-BIS(3’-INDOLYL)PYRAZOLES, ANALOGUES OF MARINE ALKALOID NORTOPSENTIN: SYNTHESIS AND ANTITUMOR PROPERTIES. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 17, 6134-6137 [http://dx.doi.org/10.1016/j.bmcl.2007.09.042].
3,5-BIS(3’-INDOLYL)PYRAZOLES, ANALOGUES OF MARINE ALKALOID NORTOPSENTIN: SYNTHESIS AND ANTITUMOR PROPERTIES
DIANA, Patrizia;CARBONE, Anna;BARRAJA, Paola;MARTORANA, Annamaria;CIRRINCIONE, Girolamo
2007-01-01
Abstract
A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91% and 41% of the tested cell lines, resp.
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