- Bioactivity and structural properties of novel synthetic analogues of the protozoan toxin climacostol
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Climacostol (5-[(2Z)-non-2-en-1-yl]benzene-1,3-diol) is a resorcinol produced by the protozoan Climacostomum virens for defence against predators. It exerts a potent antimicrobial activity against bacterial and fungal pathogens, inhibits the growth of sev
- Buonanno, Federico,Ortenzi, Claudio,Catalani, Elisabetta,Cervia, Davide,Serafini, Francesca Proietti,Picchietti, Simona,Fausto, Anna Maria,Giorgi, Simone,Lupidi, Gabriele,Rossi, Federico Vittorio,Marcantoni, Enrico,Petrelli, Dezemona
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- A straightforward diastereoselective synthesis and evaluation of climacostol, a natural product with anticancer activities
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On the basis of continued interest in plant-derived natural products as anticancer agents, a shorter and more efficient synthesis of climacostol is reported. This compound showed an anticancer activity better than that of the natural product. The improved
- Fiorini, Dennis,Giuli, Sandra,Marcantoni, Enrico,Quassinti, Luana,Bramucci, Massimo,Amantini, Consuelo,Santoni, Giorgio,Buonanno, Federico,Ortenzi, Claudio
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experimental part
p. 1550 - 1556
(2010/10/20)
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- HSP90 FAMILY PROTEIN INHIBITORS
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The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.
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Page/Page column 30
(2008/06/13)
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- HSP90 FAMILY PROTEIN INHIBITOR
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(wherein n is an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted heterocyclic-alkyl, substituted or unsubstituted aryl, -CONR7R8, -NR9R10, etc.; R2 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; R3 and R5 may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R4 and R6 may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, etc.) Provided are an Hsp90 family protein inhibitor comprising, as an active ingredient, a benzene derivative of formula (I) or a prodrug thereof or a pharmaceutically-acceptable salt thereof, etc.
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Page/Page column 50
(2008/06/13)
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