Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.


:Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four compounds: bornyl caffeate, bornyl 2-nitrocaffeate, 5-nitrocaffeic acid and 5-nitrocaffeic acid phenethyl ester (5-nitroCAPE) possess a good HIV integrase inhibitory activity, IC(50) 19.9, 26.8, 25.0 and 13.5 microM , respectively. Twelve caffeate analogues were tested by MTT assay on growth of human hepatocellular carcinoma BEL-7404, human breast MCF-7 adenocarcinoma, human lung A549 adenocarcinoma and human gastric cancer BCG823 cell lines, respectively. And the best result is IC(50) 5.5 microM for CAPE against BEL-7404.


Bioorg Med Chem Lett


Xia CN,Li HB,Liu F,Hu WX




Has Abstract


2008-12-15 00:00:00














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    abstract::3-Phenyl-3.4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Beaton H,Hamley P,Nicholls DJ,Tinker AC,Wallace AV

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  • 4,4,14 alpha-trimethyl 9 beta,19-cyclo-5 alpha-26-homocholesta-24,26-dien-3 beta-ol: a potent mechanism-based inactivator of delta 24(25)- to delta 25(27)-sterol methyl transferase.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Nes WD,He L,Mangla AT

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sansom GN,Kirk NS,Guise CP,Anderson RF,Smaill JB,Patterson AV,Kelso MJ

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Smith DG,Gribble AD,Haigh D,Ife RJ,Lavery P,Skett P,Slingsby BP,Stacey R,Ward RW,West A

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Trader DJ,Carlson EE

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Watanabe Y,Hayashida K,Saito D,Takahashi T,Sakai J,Nakata E,Kanda T,Iwai T,Hirayama S,Fujii H,Yamakawa T,Nagase H

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Qiao JX,Cheney DL,Alexander RS,Smallwood AM,King SR,He K,Rendina AR,Luettgen JM,Knabb RM,Wexler RR,Lam PY

    更新日期:2008-07-15 00:00:00

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    abstract::The natural polyether ionophore antibiotics might be important chemotherapeutic agents for the treatment of cancer. In this article, the pharmacology and anticancer activity of the polyether ionophores undergoing pre-clinical evaluation are reviewed. Most of polyether ionophores have shown potent activity against the ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章,评审


    authors: Huczyński A

    更新日期:2012-12-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Fonge H,de Saint Hubert M,Vunckx K,Rattat D,Nuyts J,Bormans G,Ni Y,Reutelingsperger C,Verbruggen A

    更新日期:2008-07-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Barber CG,Dickinson RP,Fish PV

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Peukert S,Brendel J,Pirard B,Strübing C,Kleemann HW,Böhme T,Hemmerle H

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Miretti M,Clementi R,Tempesti TC,Baumgartner MT

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Mathew SC,Ghosh N,By Y,Berthault A,Virolleaud MA,Carrega L,Chouraqui G,Commeiras L,Condo J,Attolini M,Gaudel-Siri A,Ruf J,Parrain JL,Rodriguez J,Guieu R

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Vuligonda V,Garst ME,Chandraratna RA

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Moorjani M,Zhang X,Chen Y,Lin E,Rueter JK,Gross RS,Lanier MC,Tellew JE,Williams JP,Lechner SM,Malany S,Santos M,Ekhlassi P,Castro-Palomino JC,Crespo MI,Prat M,Gual S,Díaz JL,Saunders J,Slee DH

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Alberati D,Hainzl D,Jolidon S,Krafft EA,Kurt A,Maier A,Pinard E,Thomas AW,Zimmerli D

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Hattori K,Okitsu O,Tabuchi S,Taniguchi K,Nishio M,Koyama S,Seki J,Sakane K

    更新日期:2005-07-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: He T,Wang QY,Shi JZ,Fan TY,Yan C,Huang LJ,Liu S,Hao XJ,Mu SZ

    更新日期:2014-04-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Yeung KS,Meanwell NA,Qiu Z,Hernandez D,Zhang S,McPhee F,Weinheimer S,Clark JM,Janc JW

    更新日期:2001-09-03 00:00:00

  • Chemical control of metabolically-engineered voltage-gated K+ channels.

    abstract::Metabolic oligosaccharide engineering is a powerful approach for installing unnatural glycans with unique functional groups into the glycocalyx of living cells and animals. Using this approach, we showed that K(+) channel complexes decorated with thiol-containing sialic acids were irreversibly inhibited with scorpion ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Hua Z,Lvov A,Morin TJ,Kobertz WR

    更新日期:2011-09-01 00:00:00