| 词条 | Phenylahistin |
| 释义 |
| Name = | ImageFile = phenylahistin.svg | ImageSize = | ImageAlt = | ImageName = | ImageFile1 = | ImageSize1 = | ImageAlt1 = | ImageName1 = | ImageFile2 = | ImageSize2 = | ImageAlt2 = | ImageName2 = | ImageFile3 = | ImageSize3 = | ImageAlt3 = | ImageName3 = | ImageFileL1 = | ImageSizeL1 = | ImageAltL1 = | ImageNameL1 = | ImageFileR1 = | ImageSizeR1 = | ImageAltR1 = | ImageNameR1 = | ImageFileL2 = | ImageSizeL2 = | ImageAltL2 = | ImageNameL2 = | ImageFileR2 = | ImageSizeR2 = | ImageAltR2 = | ImageNameR2 = | IUPACName = (3S,6Z)-3-Benzyl-6[5-(2-methyl-3-buten-2-yl)-1H-imidazol-4-yl]methylene2,5-piperazinedione | SystematicName = | OtherNames = |Section1={{Chembox Identifiers | 3DMet = | Abbreviations = | Beilstein = | CASNo = | CASNo_Ref = | CASNoOther = | ChEBI = 319291 | ChemSpiderID = 7974262 | DrugBank = | EC_number = | EINECS = | Gmelin = | InChI = | KEGG = | MeSHName = | PubChem = 9798496 | RTECS = | SMILES = | UNNumber = }} |Section2={{Chembox Properties | AtmosphericOHRateConstant = | Appearance = | BoilingPt = | BoilingPt_notes = | Density = | C=20 | H=22 | N=4 | O=2 | HenryConstant = | LogP = | MeltingPt = | MeltingPt_notes = | pKa = | pKb = | Solubility = | SolubleOther = | Solvent = | VaporPressure = }} |Section3={{Chembox Structure | Coordination = | CrystalStruct = | MolShape = }} |Section4={{Chembox Thermochemistry | DeltaHc = | DeltaHf = | Entropy = | HeatCapacity = }} |Section5={{Chembox Pharmacology | AdminRoutes = | Bioavail = | Excretion = | HalfLife = | Metabolism = | Legal_status = | Legal_US = | Legal_UK = | Legal_AU = | Legal_CA = | Pregnancy_category = | Pregnancy_AU = | Pregnancy_US = | ProteinBound = }} |Section6={{Chembox Explosive | DetonationV = | FrictionSens = | REFactor = | ShockSens = }} |Section7={{Chembox Hazards | AutoignitionPt = | EUClass = | ExploLimits = | ExternalSDS = | FlashPt = | LD50 = | MainHazards = | NFPA-H = | NFPA-F = | NFPA-R = | NFPA-S = | PEL = | RPhrases = | RSPhrases = | SPhrases = }} |Section8={{Chembox Related | OtherFunction_label = | OtherAnions = | OtherCations = | OtherCompounds = | OtherFunction = }} }}Phenylahistin is a metabolite produced by the fungus Aspergillus ustus[1] that belongs to a class of naturally occurring 2,5-diketopiperazines featuring a dehydrohistidine residue that exhibit important biological activities, such as anti-cancer or neurotoxic effects.[2] Phenylahistin is a microtubule binding agent that exhibits cytotoxic activities against a wide variety of tumor cell lines.[3] A series of synthetic analogs were prepared to remove the chirality and optimize biological activity. These studies led to the potent anti-tumor agent plinabulin, which is active in multidrug-resistant (MDR) tumor cell lines.[4] References1. ^{{Cite journal | title = (−)-Phenylahistin: A new mammalian cell cycle inhibitor produced by aspergillus ustus|vauthors=Kanoh K, Kohno S, Asari T, Harada T, Katada J, Muramatsu M, Kawashima H, Sekiya H, Uno I | journal = Bioorganic & Medicinal Chemistry Letters | year = 1997 | volume = 7 | issue = 22 | pages = 2847–2852 | doi = 10.1016/S0960-894X(97)10104-4}} 2. ^{{Cite journal | title = 2,5-Diketopiperazines: Synthesis, Reactions, Medicinal Chemistry, and Bioactive Natural Products | author = Borthwick AD | journal = Chemical Reviews | year = 2012 | volume = 112 | issue = 7 | pages = 3641–3716 | doi = 10.1021/cr200398y | pmid = 22575049}} 3. ^{{Cite journal | title = Antitumor activity of phenylahistin in vitro and in vivo.|vauthors=Kanoh K, Kohno S, Katada J, Hayash Y, Muramatsu M, Uno I | journal = Bioscience, Biotechnology, and Biochemistry | year = 1999 | volume = 63 | issue = 6 | pages = 1130–1133| doi = 10.1271/bbb.63.1130 | pmid = 10427703}} 4. ^{{Cite journal | title = NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent |vauthors=Nicholson B, Lloyd GK, Miller BR, Palladino MA, Kiso Y, Hayashi Y, Neuteboom ST | journal = Anticancer Drugs | year = 2006 | volume = 17 | issue = 1 | pages = 25–31| doi = 10.1097/01.cad.0000182745.01612.8a | pmid = 16317287}} 2 : Diketopiperazines|Imidazoles |
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