专利号:US-9061984-B2 优先权日:2008-08-15 标题 :Compounds related to chalcones and benzothienopyrimidines, their synthesis, and uses to treat diseases 发明人:HAMMOND GERALD B; APONTE JOSE C; GILMAN ROBERT H; SAUVAIN MICHEL HENRI AUGUSTE; VAISBERG ABRAHAM 权利人:HAMMOND GERALD B; APONTE JOSE C; GILMAN ROBERT H; SAUVAIN MICHEL HENRI AUGUSTE; VAISBERG ABRAHAM; UNIV LOUISVILLE RES FOUND; UNIV PERUMA CAYETANO HEREDIA; INST RECH POUR LE DÉVELOPPEMENT; UNIV JOHNS HOPKINS 摘要:Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).
专利号:CA-3111403-A1 优先权日:2018-09-17 标 题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease
专利号:WO-2020061106-A4 优先权日:2018-09-17 标题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease
参考标题:Synthesis Of Flavokawain Analogues And Their Anti-Neoplastic Effects On Drug-Resistant Cancer Cells Through Hsp90 Inhibition 作者:Young Ho Seo,Sun You Park |发布日期:2014.4.20 摘要:Hsp90 Is An Ubiquitous Molecular Chaperone Protein, Which Plays An Important Role In Regulating Maturation And Stabilization Of Many Oncogenic Proteins. Due To Its Potential To Simultaneously Disable Multiple Signaling Pathways, Hsp90 Represents Great Promise As A Therapeutic Target Of Cancer. In This Study, We Synthesized Flavokawain Analogues And Evaluated Their Biological Activities Against Drug-Resistant Cancer Cells. The Study Indicated That Compound 1I Impaired The Growth Of Gefitinib-Resistant Non-Small Cell Lung Cancer (H1975), Down-Regulated The Expression Of Hsp90 Client Proteins Including Egfr, Her2, Met, Akt And Cdk4, And Upregulated The Expression Of Hsp70. The Result Strongly Suggested That Compound 1I Inhibited The Proliferation Of Cancer Cells Through Hsp90 Inhibition. Overall, Compound 1I Could Serve As A Potential Lead Compound To Overcome The Drug Resistance In Cancer Chemotherapy.
合成参考文献
参考文献:10.1107/s1600536810042674 摘要:Sirat HM, Feng YS, Hazni H, Awang K, Ng SW. (E)-1-(2-Hy-droxy-4,6-dimeth-oxy-phen-yl)-3-(4-meth-oxy-phen-yl)prop-2-en-1-one from Kaempferia rotunda Val. Acta Crystallogr Sect E Struct Rep Online. 2010 Oct 30;66(Pt 11):o2944.