Trogden Bridget G, Kim Sung Hoon, Lee Shuyi, Katzenellenbogen John A
Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.
Bioorg Med Chem Lett. 2009 Jan 15;19(2):485-8. doi: 10.1016/j.bmcl.2008.11.043. Epub 2008 Nov 18.
To create ligands for the estrogen receptor that contain pendant groups for tethering to a poly(amido)amine (PAMAM) dendrimer, we have explored a class of N-substituted 2-phenyl indoles. Attachment of tethers of different length and chemical nature to this non-steroidal indole scaffold gave high affinity ligand-tether conjugates that can be easily functionalized. To further explore the utility of this system, an indole-conjugated dendrimer was prepared and evaluated as an estrogen receptor ligand.
为了制备用于雌激素受体的配体，这些配体含有用于连接到聚（酰胺）胺（PAMAM）树枝状大分子上的侧基，我们研究了一类N-取代的2-苯基吲哚。将不同长度和化学性质的连接基连接到这种非甾体吲哚骨架上，得到了高亲和力的配体-连接基共轭物，且易于功能化。为了进一步探索该体系的实用性，制备了一种吲哚共轭树枝状大分子，并将其作为雌激素受体配体进行评估。
