当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, cytotoxicity and structure-activity relationship of indolizinoquinolinedione derivatives as DNA topoisomerase IB catalytic inhibitors.

Synthesis, cytotoxicity and structure-activity relationship of indolizinoquinolinedione derivatives as DNA topoisomerase IB catalytic inhibitors.

Abstract：

:Our previous studies reveal that indolizinoquinolinedione scaffold is a base to develop novel DNA topoisomerase IB (TOP1) catalytic inhibitors. In this work, twenty-three novel indolizinoquinolinedione derivatives were synthesized. TOP1-mediated relaxation, nicking and unwinding assays revealed that three fluorinated derivatives 26, 28 and 29, and one N,N-trans derivative 46 act as TOP1 catalytic inhibitors with higher TOP1 inhibition (++++) than camptothecin (+++) and without TOP1-mediated unwinding effect. MTT assay against five human cancer cell lines indicated that the highest cytotoxicity is 20 for CCRF-CEM cells, 25 for A549 and DU-145 cells, 26 for HCT116 cells, and 33 for Huh7 cells with GI50 values at nanomolar range. The drug-resistant cell assay indicated that compound 26 may mainly act to TOP1 in cells and are less of Pgp substrates. Flow cytometric analysis showed that compounds 26, 28 and 29 can obviously induce apoptosis of HCT116 cells. Moreover, the structure-activity relationship (SAR) of indolizinoquinolinedione derivatives was analyzed.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Yu Q,Yang H,Zhu TW,Yu LM,Chen JW,Gu LQ,Huang ZS,An LK

doi

10.1016/j.ejmech.2018.04.040

subject

Has Abstract

pub_date

2018-05-25 00:00:00

pages

195-207

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30374-X

journal_volume

152

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.

    abstract：:Histone deacetylase (HDAC) enzymes govern the post-translational acetylation state of lysine residues on protein substrates, leading to regulatory changes in cell function. Due to their role in cancers, HDAC proteins have emerged as promising targets for cancer treatment. Four HDAC inhibitors have been approved as ant...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.10.076

    authors： Negmeldin AT,Knoff JR,Pflum MKH

    更新日期：2018-01-01 00:00:00

  • Synthetic tumor-specific antigenic peptides with a strong affinity to HLA-A2 elicit anti-breast cancer immune response through activating CD8+ T cells.

    abstract：:Researches on tumor-associated antigen have become a hot target in immunotherapy, but it stagnated in the pre-clinical/clinical stages. Here, we developed a series of MAGE-A1-restricted antigenic peptides, which exhibited prominent inhibiting effect on specific breast cancer. Peptides were synthesized by Fmoc solid ph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112051

    authors： Shi W,Qiu Q,Tong Z,Guo W,Zou F,Feng Z,Wang Y,Huang W,Qian H

    更新日期：2020-03-01 00:00:00

  • Structural variations of piritrexim, a lipophilic inhibitor of human dihydrofolate reductase: synthesis, antitumor activity and molecular modeling investigations.

    abstract：:Piritrexim (PTX) (1), a lipophilic inhibitor of the human dihydrofolate reductase, has been evaluated as an anticancer agent. The synthesis of four structural variations (2-5) of PTX is reported. The PTX analogues 2-5 were obtained by reaction of suitable C3-building blocks with pyrimidine-2,4,6-triamine (14) or with ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.09.001

    authors： Zink M,Lanig H,Troschütz R

    更新日期：2004-12-01 00:00:00

  • Synthesis and anticancer activity of 6-heteroarylcoumarins.

    abstract：:A series of novel 7-hydroxy-8-methyl-coumarins with indole, pyrimidine, pyrazole, pyran, tetrazolo[1,5-a]pyrimidine, pyrimido[1,2-a]benzimidazol, 2-oxo-1,2-dihydropyridine and dihydropyrazolo[3,4-b]pyridine moieties at C6 position of heterocyclic core have been synthesized. Anticancer activity screening on NCI60 cell ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.021

    authors： Galayev O,Garazd Y,Garazd M,Lesyk R

    更新日期：2015-11-13 00:00:00

  • Synthesis, beta-adrenoceptor pharmacology and toxicology of S-(-)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride, a short acting beta(1)-specific antagonist.

    abstract：:The synthesis of S-(-)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride (D140S.HCl 6), a novel short acting beta(1)-specific adrenoceptor antagonist, has been described. The antagonist potency for D140S.HCl 6 has been compared with esmolol, another short acting agent, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01399-5

    authors： Jackman GP,Iakovidis D,Nero TL,Anavekar NS,Rezmann-Vitti LA,Louis SN,Mori M,Drummer OH,Louis WJ

    更新日期：2002-09-01 00:00:00

  • Synthesis and antimicrobial activities of a new series of 4-S-[4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl]mercaptoacetyl-3-arylsydnones.

    abstract：:The synthesis of some 4-S-(4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl)mercaptoacetyl-3-arylsydnones by the reaction of 3-aryl-4-bromoacetylsydnones with 6-substituted-4-amino-3-mercapto-1,2,4-triazin-5-ones is described. The IR, (1)H NMR, mass spectra and elemental analys...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.02.003

    authors： Hegde JC,Girisha KS,Adhikari A,Kalluraya B

    更新日期：2008-12-01 00:00:00

  • Synthesis of heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy)amine COX-2 inhibitors: effects on the inhibitory activity of the replacement of the cyclopentene central core with pyrazole, thiophene or isoxazole ring.

    abstract：:Several heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy)amine COX-2 inhibitors, in which the cyclopentene moiety was replaced by pyrazole, thiophene or isoxazole ring, were synthesized, in order to verify the influence of the different nature of the central core on the COX inhibitory p...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01448-4

    authors： Balsamo A,Coletta I,Guglielmotti A,Landolfi C,Mancini F,Martinelli A,Milanese C,Minutolo F,Nencetti S,Orlandini E,Pinza M,Rapposelli S,Rossello A

    更新日期：2003-02-01 00:00:00

  • Newer GABA derivatives for the treatment of epilepsy including febrile seizures: a bioisosteric approach.

    abstract：:The present study aims at design and synthesis of newer gamma-aminobutyric acid (GABA) derivatives with the combination of thiosemicarbazone and GABA pharmacophores in order to develop newer anticonvulsants. The reported compounds were designed as bioisosteric analogues of GABA semicarbazones. The structures of the sy...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.036

    authors： Ragavendran JV,Sriram D,Kotapati S,Stables J,Yogeeswari P

    更新日期：2008-12-01 00:00:00

  • Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.

    abstract：:We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment connected through a spacer of variable length which includes a 1,2,3-triazole ring. The cytotoxic activities of these compounds have been measured. Relations between structure and c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.09.053

    authors： Vilanova C,Torijano-Gutiérrez S,Díaz-Oltra S,Murga J,Falomir E,Carda M,Alberto Marco J

    更新日期：2014-11-24 00:00:00

  • The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.

    abstract：:A series of xanthine compounds derived from the previous hit 20i with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (21h) with the improved DPP-IV...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.112017

    authors： Li G,Meng B,Yuan B,Huan Y,Zhou T,Jiang Q,Lei L,Sheng L,Wang W,Gong N,Lu Y,Ma C,Li Y,Shen Z,Huang H

    更新日期：2020-02-15 00:00:00

  • Synthesis, structural characterization and in vitro biological screening of some homoleptic copper(II) complexes with substituted guanidines.

    abstract：:A series of homoleptic copper(II) complexes (1a-8a) with N,N',N″-trisubstituted guanidines, [Cu(II){PhCONHC(NHR)NPh}(2)] (where R = phenyl (1a), n-butyl (2a), sec-butyl (3a), cyclohexyl (4a), 1-naphthyl (5a), 2,4-dichlorophenyl (6a), 3,4-dichlorophenyl (7a), and 3,5-dichlorophenyl (8a)) have been synthesized and chara...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.11.029

    authors： Murtaza G,Rauf MK,Badshah A,Ebihara M,Said M,Gielen M,de Vos D,Dilshad E,Mirza B

    更新日期：2012-02-01 00:00:00

  • Discovery and optimization of phthalazinone derivatives as a new class of potent dengue virus inhibitors.

    abstract：:Using a dengue replicon cell line-based screening, we identified 3-(dimethylamino)propyl(3-((4-(4-fluorophenyl)-1-oxophthalazin-2(1H)-yl)methyl)phenyl)carbamate (10a) as a potent DENV-2 inhibitor, with an IC50 value of 0.64 μM. A series of novel phthalazinone derivatives based on hit 10a were synthesized and evaluated...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.01.008

    authors： Lu D,Liu J,Zhang Y,Liu F,Zeng L,Peng R,Yang L,Ying H,Tang W,Chen W,Zuo J,Tong X,Liu T,Hu Y

    更新日期：2018-02-10 00:00:00

  • Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma.

    abstract：:Multidrug resistance (MDR) in cancer cells is a crucial aspect to consider for a successful cancer therapy. P-gp/ABCB1, a member of ABC transporters, is involved in the main tumour MDR mechanism, responsible for the efflux of drugs and cytotoxic substances. Herein, we describe a discovery of potent selenium-containing...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112435

    authors： Ali W,Spengler G,Kincses A,Nové M,Battistelli C,Latacz G,Starek M,Dąbrowska M,Honkisz-Orzechowska E,Romanelli A,Rasile MM,Szymańska E,Jacob C,Zwergel C,Handzlik J

    更新日期：2020-08-15 00:00:00

  • Discovery of novel HSP90 inhibitors that induced apoptosis and impaired autophagic flux in A549 lung cancer cells.

    abstract：:Heat shock protein 90 (HSP90) inhibition has aroused increasing enthusiasm in antitumor strategies in recent years. According to our previous studies, we synthesized a series of coumarin pyrazoline compounds HCP1-HCP6 that might be HSP90 inhibitors. Interactions between HCP1-HCP6 and HSP90 were examined and antitumor ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.01.024

    authors： Wei Q,Ning JY,Dai X,Gao YD,Su L,Zhao BX,Miao JY

    更新日期：2018-02-10 00:00:00

  • In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity.

    abstract：:The taxane diterpneoid 2-deacetoxytaxinine J (2-DAT-J) 1 has been isolated from the bark of Himalayan yew, Taxus baccata L. spp. wallichiana in a reasonably good yield (0.1%) and its anticancer activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human kidney epithelial cell line (HEK-293) has b...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.04.022

    authors： Reddy KP,Bid HK,Nayak VL,Chaudhary P,Chaturvedi JP,Arya KR,Konwar R,Narender T

    更新日期：2009-10-01 00:00:00

  • Synthesis, antiproliferative activities, and computational evaluation of novel isocoumarin and 3,4-dihydroisocoumarin derivatives.

    abstract：:A series of novel isocoumarin derivatives were synthesized using Castro-Stephens cross-coupling. Moreover, novel 3,4-dihydroisocoumarin derivatives were obtained by catalytic hydrogenation of the corresponding isocoumarin precursors. The antiproliferative activity of all compounds was evaluated in vitro in different t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.051

    authors： Guimarães KG,de Freitas RP,Ruiz AL,Fiorito GF,de Carvalho JE,da Cunha EF,Ramalho TC,Alves RB

    更新日期：2016-03-23 00:00:00

  • Rigid aromatic linking moiety in cationic lipids for enhanced gene transfection efficiency.

    abstract：:Although numerous cationic lipids have been developed as non-viral gene vectors, the structure-activity relationship (SAR) of these materials remains unclear and needs further investigation. In this work, a series of lysine-derived cationic lipids containing linkages with different rigidity were designed and synthesiz...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.05.038

    authors： Wang B,Zhao RM,Zhang J,Liu YH,Huang Z,Yu QY,Yu XQ

    更新日期：2017-08-18 00:00:00

  • Design, synthesis, and antiviral activity of novel rutin derivatives containing 1, 4-pentadien-3-one moiety.

    abstract：:Rutin (compound 5) and some compounds (compounds 1-4 and 6) were isolated from Artemisia princeps Pamp (A. princeps Pamp.) and a series of novel rutin derivatives containing 1,4-pentadien-3-one moiety were designed and synthesized. The target compounds were characterized by proton nuclear magnetic resonance spectrosco...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.01.017

    authors： Han Y,Ding Y,Xie D,Hu D,Li P,Li X,Xue W,Jin L,Song B

    更新日期：2015-03-06 00:00:00

  • Metal complexes of retinoid derivatives with antiproliferative activity: synthesis, characterization and DNA interaction studies.

    abstract：:9-cis-Retinal thiosemicarbazone and its Co(III), Ni(II) and Cu(II) complexes are synthesized and characterized. Central Co(III) atom is in an octahedral environment while Ni(II) and Cu(II) atoms are in a square planar environment. DNA binding constants and spectroscopic data show an intercalative behavior for the nick...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.019

    authors： Bisceglie F,Baldini M,Belicchi-Ferrari M,Buluggiu E,Careri M,Pelosi G,Pinelli S,Tarasconi P

    更新日期：2007-05-01 00:00:00

  • Unveiling the mode of action of antibacterial labdane diterpenes from Alpinia nigra (Gaertn.) B. L. Burtt seeds.

    abstract：:The labdane diterpene, (E)-labda-8(17), 12-diene-15, 16-dial (compound A) and its epoxide analogue, (E)-8β, 17-Epoxylabd-12-ene-15, 16-dial (compound B) were isolated from the seeds of Alpinia nigra for the first time. The antibacterial activities of both compounds were evaluated against three Gram-positive and four G...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.05.034

    authors： Ghosh S,Indukuri K,Bondalapati S,Saikia AK,Rangan L

    更新日期：2013-08-01 00:00:00

  • Synthesis and immunofluorescence assay of a new biotinylated paclitaxel.

    abstract：:7-(5'-Biotinylamidopropanoyl)paclitaxel was synthesised by chemical methods; its immunofluorescence assay and the cell uptake experiments were performed by use of human leukemia U937 cells. The results indicate that paclitaxel is arresting cell cycle at the G(2)M phase only. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01337-5

    authors： Sambaiah T,King KY,Tsay SC,Mei NW,Hakimclahi S,Lai YK,Lieu CH,Hwu JR

    更新日期：2002-04-01 00:00:00

  • Reversal of P-gp and BCRP-mediated MDR by tariquidar derivatives.

    abstract：:With an aim to generate non-toxic, specific and highly potent multidrug resistance (MDR) modulators, a novel series of anthranilic acid amide-substituted tariquidar derivatives were synthesized. The new compounds were evaluated for their cytotoxicity toward normal human colon fibroblasts (CCD18-Co), human gastric epit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.06.049

    authors： Li XQ,Wang L,Lei Y,Hu T,Zhang FL,Cho CH,To KK

    更新日期：2015-08-28 00:00:00

  • Synthesis, characterization and in vitro biological activity studies of Cu-M (M = Cu2+, Co2+, Ni2+, Mn2+, Zn2+) bimetallic complexes.

    abstract：:Six new bimetallic complexes of the type CuCu, CuCo, CuNi, CuZn and CuMn were prepared. The structures of these complexes and the ligand have been proposed on the basis of FAB mass, elemental analysis, UV-vis, IR, EPR and CV studies. All the complexes completely cleave pBS (SK-) DNA at a concentration of 10 microM; ho...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.11.016

    authors： Rupesh KR,Deepalatha S,Krishnaveni M,Venkatesan R,Jayachandran S

    更新日期：2006-12-01 00:00:00

  • Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.

    abstract：:Wnt signaling pathway plays a critical role in numerous cellular processes, including tumor initiation, proliferation, invasion/infiltration, metastasis formation and resistance to chemotherapy. In a drug discovery project aimed at the identification of inhibitors of the canonical Wnt pathway, we selected a series of ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.03.055

    authors： Nencini A,Pratelli C,Quinn JM,Salerno M,Tunici P,De Robertis A,Valensin S,Mennillo F,Rossi M,Bakker A,Benicchi T,Cappelli F,Turlizzi E,Nibbio M,Caradonna NP,Zanelli U,Andreini M,Magnani M,Varrone M

    更新日期：2015-05-05 00:00:00

  • Fluorinated polymer emulsion systems: Construction and application in delivering genes and proteins.

    abstract：:Emulsions have shown great potential in the delivery of various types of cargoes such as nucleic acids and proteins. In this study, fluorinated polymer emulsions (PFx@PFD-n) were prepared using fluorinated polymers with different structures as surfactant in PFD emulsions under ultrasound. These polymer emulsions gave ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112799

    authors： Xiao YP,Zhang J,Liu YH,Huang Z,Yu XQ

    更新日期：2020-12-01 00:00:00

  • Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.

    abstract：:Small molecules that can restore biological function to the p53 mutants found in human cancers have been highly sought to increase the anticancer efficacy. In efforts to generate hybrid anticancer drugs that can impact two or more targets simultaneously, we designed and developed piperlongumine (PL) derivatives with a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.052

    authors： Punganuru SR,Madala HR,Venugopal SN,Samala R,Mikelis C,Srivenugopal KS

    更新日期：2016-01-01 00:00:00

  • Synthesis and in vitro anticancer activity evaluation of novel bioreversible phosphate inositol derivatives.

    abstract：:The chemistry and biology of phosphorylated inositols have become intense areas of research during the last two decades due to their involvement in various cellular signaling processes. However, the metabolic instability by phosphatases or kinases and poor penetration make it difficult to become a drug used in the cli...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.01.064

    authors： Chen W,Deng Z,Chen K,Dou D,Song F,Li L,Xi Z

    更新日期：2015-03-26 00:00:00

  • Thiazolidine-2,4-dione-based irreversible allosteric IKK-β kinase inhibitors: Optimization into in vivo active anti-inflammatory agents.

    abstract：:Selective kinase inhibitors development is a cumbersome task because of ATP binding sites similarities across kinases. On contrast, irreversible allosteric covalent inhibition offers opportunity to develop novel selective kinase inhibitors. Previously, we reported thiazolidine-2,4-dione lead compounds eliciting in vit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111955

    authors： Elkamhawy A,Kim NY,Hassan AHE,Park JE,Paik S,Yang JE,Oh KS,Lee BH,Lee MY,Shin KJ,Pae AN,Lee KT,Roh EJ

    更新日期：2020-02-15 00:00:00

  • Synthesis and pharmacological screening of derivatives of isoxazolo[4,5-d]pyrimidine.

    abstract：:A number of derivatives of isoxazolo[4,5-d]pyrimidine were prepared with structures similar to that of purine. Condensation of the hydrazide of 4-amino-5-benzoylisoxazolo-3-carboxylic acid 2 with ethyloxalyl chloride followed by cyclization gave 3-oxdiazolo-[1,3,4]-4-amino-5-benzoylisoxazole 7 which, upon cyclization ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.035

    authors： Wagner E,Al-Kadasi K,Zimecki M,Sawka-Dobrowolska W

    更新日期：2008-11-01 00:00:00

  • Synthesis and antibacterial activity of novel modified 5-O-mycaminose 14-membered ketolides.

    abstract：:A practicable method of introducing a side chain to the C-4' position of 5-O-desosamine in the 14-membered ketolides was developed. And using this method, a series of novel modified 5-O-mycaminose ketolides were synthesized. These ketolides containing 5-O-4'-carbamate mycaminose were evaluated for their in vitro antib...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.08.023

    authors： Xu Y,Chen X,Zhu D,Liu Y,Zhao Z,Jin L,Liu C,Lei P

    更新日期：2013-11-01 00:00:00