Methyl Esters of ()-Cinnamic Acid: Activity against the Plant-Parasitic Nematode and Interaction with Histone Deacetylase.

()-Cinnamaldehyde is very active against but has low persistence in soil. To circumvent this problem, esters of cinnamic acid were evaluated as a substitute for ()-cinnamaldehyde. The best results under assays with second-stage juveniles (J2) were obtained for the methyl esters of ()--fluoro- (), ()--chloro- (), and ()--bromocinnamic acid (), which showed lethal concentrations to 50% (LC) J2 of 168, 95, and 216 μg/mL, respectively.

Synthesis and evaluation of 2-carboxy indole derivatives as potent and selective anti-leukemic agents.

Despite the success achieved in the treatment of acute lymphoblastic leukemia (ALL), the search for new drugs featuring selectivity against leukemia cells and effectiveness to prevent relapsed ALL is still highly desirable. Here, we described the synthesis of several novel 3-substituted and 3,6-disubstituted-2-carboalkoxy indoles followed by the elucidation of their mechanism of action and in vivo anti-leukemia efficacy. The synthesis of 3-substituted-2-carboalkoxy indoles relied on two Heck arylations of methyl acrylate and methyl cinnamates respectively, to generate β,β-disubstituted acrylates followed by an efficient Cadogan-Sundberg reaction of these latter intermediates.