Alkylanon of phenols with 1,3-cyclohexadiene (1) has been conducted and a series of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones were screened against the proliferation of HUVEC and cancer cells. Phenol type as well as the size and occupied position of the substitute are important for the alkylating reaction and the inhibitory activity and selectivity of a compound. 2,5-Di(cyclohexen-2-yl)benzene-1,4-diol (25) bearing two cyclohexen-2-yl groups and 2-tert-butyl-5-(cyclohexen-2-yl)benzene-1,4-diol (30) bearing cyclohexen-2-yl and tert-butyl groups exhibited good selectivity against HUVEC pioliferation (IC(50)s of 2 0 and 1 4 mu M, respectively) with relatively low toxicity to ccc-HPF-1.
BENZOFURAN DERIVATIVES WITH THERAPEUTIC ACTIVITIES
申请人:Pharmos Corporation
公开号:EP1885709A2
公开(公告)日:2008-02-13
[EN] BENZOFURAN DERIVATIVES WITH THERAPEUTIC ACTIVITIES<br/>[FR] DERIVES DE BENZOFURANNE PRESENTANT DES ACTIVITES THERAPEUTIQUES
申请人:PHARMOS CORP
公开号:WO2006129318A2
公开(公告)日:2006-12-07
[EN] The present invention relates to novel benzofuran derivatives, to pharmaceutical compositions comprising same, and to methods of use thereof. Certain compounds of the invention share some pharmacological properties with cannabinoids and have a common wide range of beneficial therapeutic indications. In particular, compounds of the invention are useful as analgesic, neuroprotective, immunomodulatory and anti-inflammatory agents. [FR] La présente invention concerne de nouveaux dérivés de benzofuranne, des compositions pharmaceutiques contenant ces dérivés, et des méthodes d'utilisation de ceux-ci. Certains de ces composés possèdent plusieurs propriétés pharmacologiques communes avec les cannabinoïdes, et présentent comme ces derniers un large éventail d'indications thérapeutiques bénéfiques. Les composés décrits conviennent en particulier comme agents analgésiques, neuroprotecteurs, immunomodulateurs, et anti-inflammatoires.
VERHE R.; SCHAMP N.; DE BUYCK L.; DE KIMPE N.; SADONES M., BULL. SOC. CHIM. BELG. <BSCB-AG>, 1975, 84, NO 7, 747-759
作者:VERHE R.、 SCHAMP N.、 DE BUYCK L.、 DE KIMPE N.、 SADONES M.