CAS: 935881-37-1; (S)-N-Hydroxy-4-(3-Methyl-2-Phenylbutanamido)Benzamide

上下游产品

N-benzyloxy-4-(3-methyl-2-phenyl-butyrylamino)-benzamideN-benzyloxy-4-(3-methyl-2-phenyl-butyrylamino)-benzamide 4-amino-N-(benzyloxy)benzamide tert-butyl (4-((benzyloxy)carbamoyl)phenyl)carbamate (S)-2-phenyl-3-methylbutyric acid

📜N-Boc-4-氨基苯甲酸置于palladium On Activated Charcoal N,N-Bis(2-Oxo-3-Oxazolidinyl)Phosphoramidic Chloride,氢气,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,三氟乙酸体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,化学反应 4.0H,反应生成 (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺
参考文献:Structure-Based Optimization Of Phenylbutyrate-Derived Histone Deacetylase Inhibitors
标题:Structure-Based Optimization Of Phenylbutyrate-Derived Histone Deacetylase Inhibitors
摘要:Previously,We Developed A Strategy To Develop A Novel Class Of Histone Deacetylase (Hdac) Inhibitors By Tethering Short-Chain Fatty Acids With Zn2+-Chelating Motifs,Which Led To N-Hydroxy-4-(4-Phenylbutyryl-Amino)Benzamide (Htpb),A Hydroxamate-Tethered Phenylbutyrate Derivative With Sub-Micromolar Potency In Inhibiting Hdac Activity And Cancer Cell Proliferation. In This Study,We Carried Out Structure-Based Optimization Of Htpb By Using The Framework Generated By The Structure Of Histone Deacetylase-Like Protein (Hdlp)-Trichostatin A (Tsa) Complexes. Docking Of Htpb Into The Hdlp Binding Domain Suggested That The Hydrophobic Microenvironment Encompassed By Phe-198 And Phe-200 Could Be Exploited For Structural Optimization. This Premise Was Corroborated By The Greater Potency Of (S)-(+)-N-Hydroxy-4-(3-Methyl-2-Phenylbutyrylamino)-Benzamide [(S)-11] (Ic50 In Hdac Inhibition,16 Nm),Of Which The Isopropyl Moiety Was Favorable In Interacting With This Hydrophobic Motif. (S)-11 At Concentrations As Low As 0.1 Mu M Was Effective In Causing Histone Hyperacetylation And P21(Waf/cip1) Overexpression And Suppressing Proliferation In Cancer Cells.
DOI:10.1021/jm0503749

专利信息

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:WO-2024259049-A1
优先权日:2023-06-13
标题:Synthesis and integration of noble gas radioisotope power systems
发明人：OLESKE KATHARINE; BICKFORD JAMES A; CASEL BRIAN; MCNABB RONALD; AGHIA JOSEPH; ARLINGTON SHANE; BARRON SARA; RAMEAU JON
权利人:CHARLES STARK DRAPER LABORATORY INC
摘要:A system to generate power in a low orbit environment may include an enclosure configured to maintain a noble gas radioisotope at a threshold pressure, wherein the noble gas radioisotope generates heat at the threshold pressure, a radiator configured to maintain the generated heat at a threshold heat, and a power converter configured to convert the maintained heat to electric power.