Synthesis of a cosalane analog with an extended polyanionic pharmacophore conferring enhanced potency as an anti-HIV agent.
Synthesis of a cosalane analog with an extended polyanionic pharmacophore conferring enhanced potency as an anti-HIV agent.
复制标题
合成具有扩展聚阴离子药效团的 cosalane 类似物，增强了作为抗 HIV 药物的效力。
DOI：
10.1016/s0960-894x(98)00121-8
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发表时间：
1998
影响因子：
2.7
通讯作者：
Rice,WG
中科院分区：
文献类型：
--
作者：
Cushman,M;Insaf,S;Ruell,JA;Schaeffer,CA;Rice,WG
A novel cosalane analog having an extended polyanionic pharmacophore was synthesized in order to target specific cationic residues on the surface of CD4. The design rationale is based on a hypothetical binding model of cosalane to the surface of the protein. The new analog displayed an EC50of 0.55 μM as an inhibitor of the cytopathic effect of HIV-1rfin CEM-SS cells, which represents a significant increase in potency over cosalane itself (EC505.1 μM). Both cosalane and the new analog are inhibitors of viral entry into target cells.
