No abstract

Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. The in vitro antitumor activity of the obtained compounds was determined at the National Cancer Institute (NCI). The 5-(benzo[d][1,3]dioxol-5-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (9a) is the most prominent of the compounds due to its remarkable activity toward leukemia (RPMI-8226), renal cancer (UO-31) and prostate cancer (DU-145) cell lines with GI(50) values of 1.88, 1.91 and 1.94 µM, respectively.

No abstract

Durch Ammonolyse von Digitoxin in 75%igem wässrigem Methanol wurden zwei stereoisomere Lactolamide erhalten die jeweils thermisch zu den Lactamen (I) cyclisiert wurden.

Among a variety of 3‐aryl‐5‐(het)arylpyrazolines, e.g. (III) and (V), derivative (IIIa) exhibits important activity against various cancer cell lines with remarkable values in leukemia, renal and prostate cancer panels.