| 词条 | Alvocidib |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 457808081 | ImageFile=Flavopiridol.svg | ImageSize=200px | ImageFile1=Alvocidib ball-and-stick.png | ImageSize1=200px | IUPACName=2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4-chromenone | OtherNames=Flavopiridol, HMR 1275, L-868275 |Section1={{Chembox Identifiers | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 45AD6X575G | IUPHAR_ligand = 5680 | CASNo_Ref = {{cascite|changed|??}} | CASNo=146426-40-6 | PubChem= 5287969 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 47344 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 428690 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4450222 | KEGG = D09868 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C21H20ClNO5/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3/t12-,17+/m0/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = BIIVYFLTOXDAOV-YVEFUNNKSA-N | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB03496 | SMILES = Clc4ccccc4C=2Oc1c(c(O)cc(O)c1C(=O)C=2)[C@H]3CCN(C)C[C@H]3O | MeSHName = Flavopiridol |Section2={{Chembox Properties | Formula=C21H20ClNO5 | MolarMass=401.8402 | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= |Section3={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }}Alvocidib (INN; also known as Flavopiridol) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc. It has been studied also for the treatment of arthritis[1] and atherosclerotic plaque formation [2] The target of Flavopiridol is the positive transcription elongation factor P-TEFb.[3][4] Treatment of cells with Flavopiridol leads to inhibition of P-TEFb and the loss of mRNA production.[5][6] The compound is a semisynthetic derivative of rohitukine which was initially extracted from Aphanamixis polystachya and later from Dysoxylum binectariferum.[7][8] Orphan drug{{cquote|Tolero Pharmaceuticals Inc. announced that the FDA has granted orphan drug designation for Alvocidib, its cyclin-dependent kinase small molecule inhibitor, for the treatment of patients with acute myeloid leukemia.[9]}}References1. ^{{cite journal | vauthors = Sekine C, Sugihara T, Miyake S, Hirai H, Yoshida M, Miyasaka N, Kohsaka H | title = Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors | journal = J. Immunol. | volume = 180 | issue = 3 | pages = 1954–61 | year = 2008 | pmid = 18209094 | doi = 10.4049/jimmunol.180.3.1954}} {{Intracellular chemotherapeutic agents}}{{antineoplastic-drug-stub}}2. ^{{cite journal | vauthors = Ruef J, Meshel AS, Hu Z, Horaist C, Ballinger CA, Thompson LJ, Subbarao VD, Dumont JA, Patterson C | title = Flavopiridol inhibits smooth muscle cell proliferation in vitro and neointimal formation In vivo after carotid injury in the rat | journal = Circulation | volume = 100 | issue = 6 | pages = 659–65 | year = 1999 | pmid = 10441105 | doi = 10.1161/01.cir.100.6.659}} 3. ^{{cite journal | vauthors = Chao SH, Fujinaga K, Marion JE, Taube R, Sausville EA, Senderowicz AM, Peterlin BM, Price DH | title = Flavopiridol inhibits P-TEFb and blocks HIV-1 replication | journal = J. Biol. Chem. | volume = 275 | issue = 37 | pages = 28345–8 | year = 2000 | pmid = 10906320 | doi = 10.1074/jbc.C000446200 }} 4. ^{{cite journal | vauthors = Chao SH, Price DH | title = Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo | journal = J. Biol. Chem. | volume = 276 | issue = 34 | pages = 31793–9 | year = 2001 | pmid = 11431468 | doi = 10.1074/jbc.M102306200 }} 5. ^{{cite journal | vauthors = Cheng B, Li T, Rahl PB, Adamson TE, Loudas NB, Guo J, Varzavand K, Cooper JJ, Hu X, Gnatt A, Young RA, Price DH | title = Functional association of Gdown1 with RNA polymerase II poised on human genes | journal = Mol. Cell | volume = 45 | issue = 1 | pages = 38–50 | year = 2012 | pmid = 22244331 | pmc = 3259526 | doi = 10.1016/j.molcel.2011.10.022 }} 6. ^{{cite journal | vauthors = Rahl PB, Lin CY, Seila AC, Flynn RA, McCuine S, Burge CB, Sharp PA, Young RA | title = c-Myc regulates transcriptional pause release | journal = Cell | volume = 141 | issue = 3 | pages = 432–45 | year = 2010 | pmid = 20434984 | pmc = 2864022 | doi = 10.1016/j.cell.2010.03.030 }} 7. ^{{cite journal|last1=Harmon|first1=AD|last2=Weiss|first2=U|last3=Silverton|first3=JV|title=The structure of rohitukine, the main alkaloid of Amoora rohituka (syn.Aphanamixis polystachya) (Meliaceae)|journal=Tetrahedron Lett.|date=1979|volume=20|issue=1|pages=721–724|doi=10.1016/S0040-4039(01)93556-7}} 8. ^{{cite journal|last1=Lakdawala|first1=AD|last2=Shirole|first2=MV|last3=Mandrekar|first3=SS|last4=Dohadwalla|first4=AN|title=Immunopharmacological potential of rohitukine: a novel compound isolated from the plant Dysoxylum binectariferum|journal=Asia Pac J Pharmcol.|date=1988|volume=3|issue=1|pages=91–98|accessdate=}} 9. ^http://www.healio.com/hematology-oncology/hematologic-malignancies/news/online/%7B74c6a69e-4529-400d-98e9-d5ee6c602122%7D/fda-grants-orphan-drug-status-to-alvocidib-for-aml 4 : Experimental cancer drugs|Chromones|Protein kinase inhibitors|Orphan drugs |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。