[EN] NOVEL ESTROGEN RECEPTOR LIGANDS<br/>[FR] NOUVEAUX LIGANDS POUR RÉCEPTEURS D'OESTROGÈNES
申请人:KAROBIO AB
公开号:WO2013017654A1
公开(公告)日:2013-02-07
Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
The invention is directed to physiologically active compounds of the general formula (Ix)
and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
A method of deterring biofouling of a surface comprising attaching an adduct having formula (I) or noradrenalin to the surface. Formula (I) being defined as compounds that have the formula A-L-R wherein A is i) a C6 or C10 substituted aryl ring, or ii) a C1-C9 substituted or unsubstituted heteroaryl ring: L is a linking group, and R is a primary amino moiety comprising unit.
[EN] PYRAZOLE-OXAZOLIDINONE COMPOUND FOR ANTI-HEPATITIS B VIRUS<br/>[FR] COMPOSÉ PYRAZOLE-OXAZOLIDINONE POUR LUTTER CONTRE LE VIRUS DE L'HÉPATITE B<br/>[ZH] 抗乙肝病毒的吡唑-噁唑烷酮类化合物
Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors
作者:Qun Sun、Barbara Gatto、Chiang Yu、Angela Liu、Leroy F. Liu、Edmond J. LaVoie
DOI:10.1021/jm00018a024
日期:1995.9
The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.