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Identification of a novel polyfluorinated compound as a lead to inhibit the human enzymes aldose reductase and AKR1B10: structure determination of both ternary complexes and implications for drug
Comparison of the two structures of the AKR1B10-NADP(+)-JF0064 complex has unveiled some important hints for subsequent structure-based drug-design efforts. Expand
Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.
A polybrominated diphenyl ether naturally occurring in a marine sponge was found to inhibit recombinant human ALR2 with an IC(50) of 6.4 microM, and a crucial bromine atom is assessed that distinguishes the active lead compound from a much less active close natural analogue. Expand
Diazonamides C–E, new cytotoxic metabolites from the ascidian Diazona sp.
Abstract Three new macrocyclic peptides, diazonamides C–E ( 1 – 3 ), were isolated together with the previously reported diazonamides A ( 4 ) and B ( 5 ) from samples of the marine ascidian DiazonaExpand
Isolation and structures of pipecolidepsins A and B, cytotoxic cyclic depsipeptides from the Madagascan sponge Homophymia lamellosa.
Two new cyclic depsipeptides, pipecolidepsins A and B, have been isolated from the sponge Homophymia lamellosa collected off the coast of Madagascar and displayed cytotoxic activity against a panel of different human tumor cell lines. Expand
Structural Determinants of the Selectivity of 3‐Benzyluracil‐1‐acetic Acids toward Human Enzymes Aldose Reductase and AKR1B10
This selectivity also occurs in the cell, which enables the development of a more efficient drug design strategy: compound 3 prevents sorbitol accumulation in human retinal ARPE‐19 cells, whereas 4 stops proliferation in human lung cancer NCI‐H460 cells. Expand
1,5-Diazacyclohenicosane, a New Cytotoxic Metabolite from the Marine Sponge Mycale sp
A new cyclic diamine, 1,5-diazacyclohenicosane (1), was isolated from samples of the marine sponge Mycale sp. collected at Lamu Island (Kenya). Its structure was determined by a combination ofExpand
Isolation and first total synthesis of PM050489 and PM060184, two new marine anticancer compounds.
This work describes the first isolation, structural elucidation and total synthesis of two totally new polyketides isolated from the Madagascan sponge Lithoplocamia lithistoides, which show antimitotic properties in human tumor cells lines at subnanomolar concentrations and display a distinct inhibition mechanism on microtubules. Expand
Netamines A–G: seven new tricyclic guanidine alkaloids from the marine sponge Biemna laboutei
Abstract In our continuing program to identify bioactive compounds from marine invertebrates, the MeOH/EtOAc (1:1) extract of three collections of the Madagascar sponge, Biemna laboutei, was found toExpand
Synthesis and structure-activity relationships of 1,5-diazaanthraquinones as antitumour compounds.
1,5-Diazaanthraquinone derivatives were synthesized employing single and double hetero Diels-Alder strategies and showed IC(50) values in the 10(-8)M range for human lung carcinoma and human melanoma, which makes them attractive candidates for further development as anticancer agents. Expand
Plumisclerin A, a diterpene with a new skeleton from the soft coral Plumigorgia terminosclera.
A novel compound, named plumisclerin A, was isolated from samples of the soft coral Plumigorgia terminosclera collected at Mayotte Island, and displayed in vitro cytotoxicity against selected cancer cell lines. Expand