Synthesis and bioassay evaluation of 1-(4-substitutedideneaminooxymethyl)-phenyl-3-(2,6-difluorobenzoyl)ureas
摘要:
A variety of novel 1-(4-substitutedideneaminooxymethyl)-phenyl-3-(2,6-difluorobenzoyl)ureas were designed and synthesized by the reaction of 4-substitutedideneaminooxyrnethyl aniline with 2,6-difluorobenzoyl isocyanates in good yields. The title compounds were soluble in most organic solvents, which should make them easier to use. The preliminary bioassay showed that some of the title compounds show excellent insecticidal activity against Mythimna separata at the dosage of 25 mg kg(-1) and moderate insecticidal activity against Nephotettix cincticeps at the dosage of 500 mg kg(-1). Toxicity assays indicated that these title compounds cause in M. separata and N. cincticeps such symptoms of toxicity as discolouration, and weight loss, and cessation of feeding and lethal. One title compound exhibited acaricidal activity against Tetranychus urticae. (c) 2007 Elsevier Ltd. All rights reserved.
CEPHALOTAXUS ESTERS, METHODS OF SYNTHESIS, AND USES THEREOF
申请人:Gin David
公开号:US20110071097A1
公开(公告)日:2011-03-24
The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.