title: Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.
abstract: The first direct activator of BAX, a pro-apoptotic member of the BCL-2 family, has been recently identified. Herein, a structure-based lead optimization turned out into a small series of analogues, where 8 is the most potent compound published so far. 8 was used as pharmacological tool to ascertain, for the first time, the anticancer potential of BAX direct activators and the obtained results would suggest that BAX direct activators are potential future anticancer drugs rather than venoms.
authors: Dipartimento di Farmacia, Università di Napoli "Federico II" , via D. Montesano 49, 80131 Naples, Italy.
authors: Mariano
authors: M
authors: Stornaiuolo
authors: Giuseppe
authors: G
authors: La Regina
authors: Sara
authors: S
authors: Passacantilli
authors: Gianluca
authors: G
authors: Grassia
authors: Antonio
authors: A
authors: Coluccia
authors: Valeria
authors: V
authors: La Pietra
authors: Mariateresa
authors: M
authors: Giustiniano
authors: Hilde
authors: H
authors: Cassese
authors: Salvatore
authors: S
authors: Di Maro
authors: Diego
authors: D
authors: Brancaccio
authors: Sabrina
authors: S
authors: Taliani
authors: Armando
authors: A
authors: Ialenti
authors: Romano
authors: R
authors: Silvestri
authors: Claudia
authors: C
authors: Martini
authors: Ettore
authors: E
authors: Novellino
authors: Luciana
authors: L
authors: Marinelli
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005455:Fluorescent Antibody Technique; D006801:Humans; D006835:Hydrazones / Q000737:chemistry* / Q000494:pharmacology*; D015151:Immunoblotting; D047468:Immunoprecipitation; D019169:Jurkat Cells; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D008928:Mitochondria / Q000187:drug effects / Q000378:metabolism; D008958:Models, Molecular; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D051028:bcl-2-Associated X Protein / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: C000598567:1-(4'-(dimethylamino)-5-hydroxy-(1,1'-biphenyl)-3-yl)-4-(2-(2-ethoxyphenyl)hydrazono)-3-methyl-1H-pyrazol-5(4H)-one; D000970:Antineoplastic Agents; D006835:Hydrazones; D011720:Pyrazoles; D051028:bcl-2-Associated X Protein