CAS: 149204-42-2; Kahalalide F

该化合物是源自海洋软体埃利西亚叶卡西娅叶酸化物的循环性排piptide,以其潜在的药理特性著称;该化合物呈现出一个复杂的结构,其特点是一系列氨基酸残留物和独特的内酯联系,有助于其生物活动;Kahalide F由于对各种癌症细胞线的细胞毒性效应及其作为抗炎剂的潜力表现出来,因此对药用化学领域产生了兴趣;该物质也因其抑制某些酶的能力而得到注意,这些酶在治疗作用中可能发挥作用;此外,Kahalalide F已经就其对骨质疏松症和细胞循环调节的影响进行了研究,使其成为癌症治疗进一步研究的候选物;它独特的海洋来源和结构特征突出了天然产品在药物发现和开发中的重要性;然而,为了充分了解其在临床环境中的行动和潜在应用机制,有必要开展进一步研究.

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      专利信息


      专利号:US-9353057-B2
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
      发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
      权利人:XENOPORT INC
      摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

      专利号:US-8734846-B2
      优先权日:2008-06-16
      标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
      发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
      权利人:BIND BIOSCIENCES INC
      摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

      专利号:US-2013035307-A1
      优先权日:2010-01-26
      标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
      发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
      权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
      摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:US-2008214827-A1
      优先权日:2004-02-03
      标 题:Synthesis of Cyanoimino-Benzoimidazoles
      发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
      权利人:EURO CELTIQUE SA
      摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

      专利号:US-9220714-B2
      优先权日:2006-03-16
      标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
      发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
      权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
      摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

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      合成参考文献


      参考文献:10.1021/np070508g
      摘要:Rao KV, Na M, Cook JC, Peng J, Matsumoto R, Hamann MT. Kahalalides V–Y Isolated from a Hawaiian Collection of the Sacoglossan Mollusk Elysia rufescens. J. Nat. Prod. 2008 Apr 12;71(5):772–8. doi: 10.1021/np070508g.
      摘要:Nuijen B, Bouma M, Manada C, Jimeno JM, Bult A, Beijnen JH. In vitro hemolysis and buffer capacity studies with the novel marine anticancer agent kahalalide F and its reconstitution vehicle cremophor EL/ethanol. PDA J Pharm Sci Technol. 2001 Jul;55(4):223–9.
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