title: Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents.
abstract: A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1(IIIB) in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC(50) values of 0.012, 0.025, 0.088 and 0.162nM, respectively.
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China. yphe@ynu.edu.cn
authors.forename: Yan-Ping
authors.initials: YP
authors.lastname: He
authors.forename: Jin
authors.initials: J
authors.lastname: Long
authors.forename: Shui-Shuan
authors.initials: SS
authors.lastname: Zhang
authors.forename: Cong
authors.initials: C
authors.lastname: Li
authors.forename: Christopher Cong
authors.initials: CC
authors.lastname: Lai
authors.forename: Chun-Sheng
authors.initials: CS
authors.lastname: Zhang
authors.forename: Da-Xiong
authors.initials: DX
authors.lastname: Li
authors.forename: De-Hua
authors.initials: DH
authors.lastname: Zhang
authors.forename: Hua
authors.initials: H
authors.lastname: Wang
authors.forename: Qing-Qing
authors.initials: QQ
authors.lastname: Cai
authors.forename: Yong-Tang
authors.initials: YT
authors.lastname: Zheng
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000821:virology; D019829:Nevirapine / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D015215:Zidovudine / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D011743:Pyrimidines; D015215:Zidovudine; D019829:Nevirapine