title: Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors.
abstract: A novel series of naphthyl phenyl ether analogues (NPEs) have been synthesized and evaluated for their in vitro activities against HIV in C8166 cells. Most of the compounds exhibited moderate to excellent anti-HIV activities. Among them the most active compound 12o showed excellent activities against wild-type HIV-1 with an EC(50) value of 4.60 nM, along with moderate activities against the double mutant strain HIV-1(IIIB) A17 (K103N+Y181C) and HIV-2 strain ROD with an EC(50) value of 0.82 and 4.40 μM, respectively. Preliminary structure-activity relationship (SAR) among the newly synthesized NPEs was also investigated.
authors.affiliation: Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
authors.forename: Shuang-Xi
authors.initials: SX
authors.lastname: Gu
authors.forename: Xuan
authors.initials: X
authors.lastname: Zhang
authors.forename: Qiu-Qin
authors.initials: QQ
authors.lastname: He
authors.forename: Liu-Meng
authors.initials: LM
authors.lastname: Yang
authors.forename: Xiao-Dong
authors.initials: XD
authors.lastname: Ma
authors.forename: Yong-Tang
authors.initials: YT
authors.lastname: Zheng
authors.forename: Shi-Qiong
authors.initials: SQ
authors.lastname: Yang
authors.forename: Fen-Er
authors.initials: FE
authors.lastname: Chen
mesh_terms: D002460:Cell Line; D004987:Ethers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004987:Ethers; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase