Pharmacophore-based small molecule CXCR4 ligands

详细信息	查看全文 | 推荐本文 |

• 作者：Tetsuo Narumi^a ; Tomohiro Tanaka^a ; Chie Hashimoto^a ; Wataru Nomura^a ; Haruo Aikawa^a ; Akira Sohma^a ; Kyoko Itotani^a ; Miyako Kawamata^b ; Tsutomu Murakami^b ; Naoki Yamamoto^c ; Hirokazu Tamamura^a ; ^{tamamura.mr@tmd.ac.jp}
• 关键词：HIV entry inhibitors ; Chemokine receptor ; AIDS ; Low molecular weight CXCR4 ligands
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：4169-4172
• 文件大小：464 K

摘要

Low molecular weight CXCR4 ligands were developed based on the peptide T140, which has previously been identified as a potent CXCR4 antagonist. Some compounds with naphthyl, fluorobenzyl and pyridyl moieties as pharmacophore groups in the molecule showed significant CXCR4-binding activity and anti-HIV activity. Structure-activity relationships were studied and characteristics of each of these three moieties necessary for CXCR4 binding were defined. In this way, CXCR4 ligands with two types of recognition modes for CXCR4 have been found.