Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents

Ursolic acid derivatives induce cell cycle arrest and apoptosis in NTUB1 cells associated with reactive oxygen species

“…Compound 1 in acetone reacted with K 2 CO 3 and various alkyl halides to afford different esters (2-11 and 19) (Scheme 1). The hydroxyl group at C-3 in the ring A was treated with various anhydrides to form different esters (12)(13)(14)(15)(16)(17) (Scheme 2). Compound 1 was oxidized to the 3-keto compound 18 with CrO 3 in DMF and the treatment of 3-oxo-derivative 18 with mchloroperbenzoic acid (m-CPBA) afford lactone 20.…”

Design, synthesis and pharmacophoric model building of novel substituted nicotinic acid hydrazones with potential antiproliferative activity

“…Due to its synthetic and biological versatility, in recent years investigations on compounds containing hydrazide or hydrazone moieties are attractive target compounds for new drug development, because of their potentially biological activities involving antiproliferative activities (Kamal et al, 2007;Onnis et al, 2009). Several studies have been devoted to the antiproliferative activity of aroylhydrazone derivatives (Easmon et al, 2006;Putt et al 2006;Vogel et al, 2008;Xia et al, 2008;Onnis et al, 2009). It has been suggested that the antiproliferative activity of these hydrazones may be attributed to inhibition of kinases (Hellmuth et al, 2008;Xu et al, 2008;Horiuchi et al 2009), generation of radicals, and dissipation of the mitochondrial membrane potential (Hofmann et al, 2009).…”

Synthesis and evaluation of anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines

“…For example aroyl hydrazones of 2-phenylindole-3-carbaldehydes were capable to cause cell cycle arrest accompanied by apoptosis in MDA-MB 231 and MCF-7 breast cancer cells. 4 Furthermore the aroylhydrazone PAC-1 directly activates procaspase-3 to caspase-3 in vitro and induces apoptosis in cancerous cells isolated from primary colon tumors in a manner directly proportional to the concentration of procaspase-3 inside these cells. 5 A variety of hydrazones demonstrated their antiproliferative activity through inhibition of kinases.…”