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排序方式: 共有43条查询结果,搜索用时 15 毫秒
1.
Purandare AV Wan H Laing N Benbatoul K Vaccaro W Poss MA 《Bioorganic & medicinal chemistry letters》2004,14(18):4701-4704
Synthesis and in vitro characterization of novel, lactam boronic acid based, selective, and rapidly reversible inhibitor 14 of the 20S-proteasome is presented. 相似文献
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Purandare AV Wan H Somerville JE Burke C Vaccaro W Yang X McIntyre KW Poss MA 《Bioorganic & medicinal chemistry letters》2007,17(3):679-682
The design, synthesis, and SAR studies of 'core' variations led to identification of novel, selective, and potent small molecule antagonist (22) of the CC chemokine receptor-4 (CCR4) with improved in vitro activity and liability profile. Compound 22 was efficacious in a murine allergic inflammation model (ED50 approximately 10 mg/kg). 相似文献
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A study of bacterial surface oligosaccharides were investigated among
different strains of Neisseria gonorrhoeae to correlate structural features
essential for binding to the MAb 2C7. This epitope is widely expressed and
conserved in gonococcal isolates, characteristics essential to an effective
candidate vaccine antigen. Sample lipooligosaccharides (LOS), was prepared
by a modification of the hot phenol-water method from which de-O-acetylated
LOS and oligosaccharide (OS) components were analyzed by ES-MS-CID-MS and
ES-MSnin a triple quadrupole and an ion trap mass spectrometer,
respectively. Previously documented natural heterogeneity was apparent from
both LOS and OS preparations which was admixed with fragments induced by
hydrazine and mild acid treatment. Natural heterogeneity was limited to
phosphorylation and antenni extensions to the alpha-chain. Mild acid
hydrolysis to release OS also hydrolyzed the beta(1-->6) glycosidic
linkage of lipid A. OS structures were determined by collisional and
resonance excitation combined with MS and multistep MSn which provided
sequence information from both neutral loss, and nonreducing terminal
fragments. A comparison of OS structures, with earlier knowledge of MAb
binding, enzyme treatment, and partial acid hydrolysis indicates a generic
overlapping domain for 2C7 binding. Reoccurring structural features include
a Hepalpha(1-->3)Hepbeta(1-->5)KDO trisaccharide core branched on the
nonreducing terminus (Hep-2) with an alpha(1-->2) linked GlcNAc
(gamma-chain), and an alpha-linked lactose (beta-chain) residue. From the
central heptose (Hep-1), a beta(1-->4) linked lactose (alpha-chain),
moiety is required although extensions to this residue appear unnecessary.
相似文献
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Purandare AV Chen Z Huynh T Pang S Geng J Vaccaro W Poss MA Oconnell J Nowak K Jayaraman L 《Bioorganic & medicinal chemistry letters》2008,18(15):4438-4441
This study reports the identification and Hits to Leads optimization of inhibitors of coactivator associated arginine methyltransferase (CARM1). Compound 7b is a potent, selective inhibitor of CARM1. 相似文献
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Tram Huynh Zhong Chen Suhong Pang Jieping Geng Tiziano Bandiera Simona Bindi Paola Vianello Fulvia Roletto Sandrine Thieffine Arturo Galvani Wayne Vaccaro Michael A. Poss George L. Trainor Matthew V. Lorenzi Marco Gottardis Lata Jayaraman Ashok V. Purandare 《Bioorganic & medicinal chemistry letters》2009,19(11):2924-2927
Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1). 相似文献
10.
Purandare AV Wan H Gao A Somerville J Burke C Vaccaro W Yang X McIntyre KW Poss MA 《Bioorganic & medicinal chemistry letters》2006,16(1):204-207
The design, synthesis, and activity of novel and selective small molecule antagonists of the CC chemokine receptor-4 (CCR4) are presented. Compound 8c was efficacious in a murine allergic inflammation model (ED(50) 30 mg/kg). 相似文献