title: Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues.
abstract: Two 1-thia-DCK analogues (9a and 9b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC(50) value of 0.00012 microM and therapeutic index of 1408000. Compound 9b was less active with EC(50) and TI values of 3.11 microM and 62.3, respectively. The bioassay results indicated that thia-DCK analogues merit attention as potential HIV-1 inhibitors.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China. pxia@shmu.edu.cn
authors.forename: Peng
authors.initials: P
authors.lastname: Xia
authors.forename: Zhi-Jian
authors.initials: ZJ
authors.lastname: Yin
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.forename: Beina
authors.initials: B
authors.lastname: Zhang
authors.forename: Yi
authors.initials: Y
authors.lastname: Xia
authors.forename: Zheng-Yu
authors.initials: ZY
authors.lastname: Yang
authors.forename: Nicole
authors.initials: N
authors.lastname: Kilgore
authors.forename: Carl
authors.initials: C
authors.lastname: Wild
authors.forename: Susan L
authors.initials: SL
authors.lastname: Morris-Natschke
authors.forename: Kuo-Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002164:Camphor / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D013601:T-Lymphocytes / Q000187:drug effects / Q000821:virology; D014779:Virus Replication / Q000187:drug effects
chemical_list: C479985:3'R,4'R-di-O-(-)-camphanoyl-(+)-cis-khellactone; D019380:Anti-HIV Agents; D007783:Lactones; D002164:Camphor