title: Cytotoxic aaptamine derivatives from the South China Sea sponge Aaptos aaptos.
abstract: Nine new aaptamine derivatives (1-9), together with three known related compounds (10-12), have been isolated from the South China Sea sponge Aaptos aaptos. The structures of all compounds were unambiguously elucidated on the basis of spectroscopic analyses. Structurally, compound 1 possesses a piperidinyl group fused to a demethyl(oxy)aaptamine moiety, whereas compounds 3-6 share an imidazole-fused 1H-benzo[de][1,6]naphthyridin-2(4H)-one skeleton. The cytotoxic activities of the compounds were evaluated against various human cancer cell lines, and compounds 2, 8, 11, and 12 showed potent cytotoxicities against HL60, K562, MCF-7, KB, HepG2, and HT-29 cells, with IC50 values in the range of 0.03 to 8.5 μM.
authors.affiliation: Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University , 415 Fengyang Road, Shanghai 200003, People's Republic of China.
authors.forename: Hao-Bing
authors.initials: HB
authors.lastname: Yu
authors.forename: Fan
authors.initials: F
authors.lastname: Yang
authors.forename: Fan
authors.initials: F
authors.lastname: Sun
authors.forename: Guo-Yi
authors.initials: GY
authors.lastname: Ma
authors.forename: Jian-Hong
authors.initials: JH
authors.lastname: Gan
authors.forename: Wen-Zhen
authors.initials: WZ
authors.lastname: Hu
authors.forename: Bing-Nan
authors.initials: BN
authors.lastname: Han
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Jiao
authors.forename: Hou-Wen
authors.initials: HW
authors.lastname: Lin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D002681:China; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D019073:HT29 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D020014:K562 Cells; D015394:Molecular Structure; D009287:Naphthyridines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D019906:Nuclear Magnetic Resonance, Biomolecular; D009792:Oceans and Seas; D011161:Porifera / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D009287:Naphthyridines; C043986:aaptamine