- Structural Determinants for Affinity Enhancement of a Dual Antagonist Peptide Entry Inhibitor of Human Immunodeficiency Virus Type-1.
[作者:Gopi, Hosahudya;Umashankara, M.;Pirrone, Vanessa;LaLonde, Judith;Madani, Navid;Tuzer, Ferit;Baxter, Sabine;Zentner, Isaac;Cocklin, Simon;Jawanda, Navneet;Miller, Shendra R.;Schoen, Arne;Klein, Jeffrey C.;Freire, Ernesto;Krebs, Fred C.;Smith, Amos B.;Sodro,期刊:Journal of Medicinal Chemistry, 页码:2638-2647 , 文章类型: 研究论文,,卷期:2008年51-9]
- Structure-activity correlations were investigated for substituted peptide conjugates that function as dual receptor site antagonists of HIV-1 gp120. A series of peptide conjugates were constructed via click reaction of ...
- 2-(6-Aryl-3(Z)-hexen-1,5-diynyl)anilines as a New Class of Potent Antitubulin Agents.
[作者:Lo, Yu-Hsiang;Lin, Ching-Chih;Lin, Chi-Fong;Lin, Ying-Ting;Duh, Tsai-Hui;Hong, Yi-Ren;Yang, Sheng-Huei;Lin, Shinne-Ren;Yang, Shyh-Chyun;Chang, Long-Sen;Wu, Ming-Jung;,期刊:Journal of Medicinal Chemistry, 页码:2682-2688 , 文章类型: 研究论文,,卷期:2008年51-9]
- Several synthesized compds. displayed significant GI50 values of showed the most potent growth inhibition activity. Compd. I also arrested cancer cells in the G2/M phase and in low concn. reduced a significant percentag...
- Comparing In Vitro and In Vivo Activity of 2'-O-[2-(Methylamino)-2-oxoethyl]- and 2'-O-Methoxyethyl-Modified Antisense Oligonucleotides.
[作者:Prakash, Thazha P.;Kawasaki, Andrew M.;Wancewicz, Edward V.;Shen, Lijiang;Monia, Brett P.;Ross, Bruce S.;Bhat, Balkrishen;Manoharan, Muthiah;,期刊:Journal of Medicinal Chemistry, 页码:2766-2776 , 文章类型: 研究论文,,卷期:2008年51-9]
- A no. of 2'-O-modified antisense oligonucleotides have been reported for their potential use in oligonucleotide-based therapeutics. To date, most of the in vivo data has been generated for 2'-O-MOE (2'-O-methoxyethyl)- ...
- De Novo Design of Nonpeptidic Compounds Targeting the Interactions between Interferon-a and its Cognate Cell Surface Receptor.
[作者:Bello, Angelica M.;Bende, Tanushree;Wei, Lianhu;Wang, Xiaoyang;Majchrzak-Kita, Beata;Fish, Eleanor N.;Kotra, Lakshmi P.;,期刊:Journal of Medicinal Chemistry, 页码:2734-2743 , 文章类型: 研究论文,,卷期:2008年51-9]
- Type 1 interferons (IFN) bind specifically to the corresponding receptor, IFNAR. Agonists and antagonists for IFNAR have potential therapeutic value in the treatment of viral infections and systemic lupus erythematosus,...
- (3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2, 4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor wit
[作者:Ahmad, Saleem;Madsen, Cort S.;Stein, Philip D.;Janovitz, Evan;Huang, Christine;Ngu, Khehyong;Bisaha, Sharon;Kennedy, Lawrence J.;Chen, Bang-Chi;Zhao, Rulin;Sitkoff, Doree;Monshizadegan, Hossain;Yin, Xiaohong;Ryan, Carol S.;Zhang, Rongan;Giancarli, Mary;Bi,期刊:Journal of Medicinal Chemistry, 页码:2722-2733 , 文章类型: 研究论文,,卷期:2008年51-9]
- 3-Hydroxy-3-methylglutaryl coenzyme-A reductase (HMGR) inhibitors, more commonly known as statins, represent the gold std. in treating hypercholesterolemia. Although statins are regarded as generally safe, they are know...
- Synthesis and Biological Activity of Fluorinated Combretastatin Analogues.
[作者:Alloatti, Domenico;Giannini, Giuseppe;Cabri, Walter;Lustrati, Isabella;Marzi, Mauro;Ciacci, Andrea;Gallo, Grazia;Tinti, M. Ornella;Marcellini, Marcella;Riccioni, Teresa;Guglielmi, Mario B.;Carminati, Paolo;Pisano, Claudio;,期刊:Journal of Medicinal Chemistry, 页码:2708-2721 , 文章类型: 研究论文,,卷期:2008年51-9]
- With the aim of understanding the influence of fluorine on the double bond of the cis-stilbene moiety of combretastatin derivs. and encouraged by a preliminary mol. modeling study showing a different biol. environment on...
- Design and Synthesis of Peripherally Restricted Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists.
[作者:Tamayo, Nuria;Liao, Hongyu;Stec, Markian M.;Wang, Xianghong;Chakrabarti, Partha;Retz, Dan;Doherty, Elizabeth M.;Surapaneni, Sekhar;Tamir, Rami;Bannon, Anthony W.;Gavva, Narender R.;Norman, Mark H.;,期刊:Journal of Medicinal Chemistry, 页码:2744-2757 , 文章类型: 研究论文,,卷期:2008年51-9]
- Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clin. utility for the treatment of chronic nociceptive and neuropathic pain. The authors recently advanced a TRPV1 antagonist, AMG 517, into ...
- Discovery of subnanomolar arginine-glycine-aspartate-based aVb3/aVb5 integrin binders embedding 4-aminoproline residues.
[作者:[Erratum to document cited in CA148:427174]. Zanardi, Franca;Burreddu, Paola;Rassu, Gloria;Auzzas, Luciana;Battistini, Lucia;Curti, Claudio;Sartori, Andrea;Nicastro, Giuseppe;Menchi, Gloria;Cini, Nicoletta;Bottoncetti, Anna;Raspanti, Silvia;Casiraghi, Gio,期刊:Journal of Medicinal Chemistry, 页码:2870-2870 , 文章类型: 研究论文,,卷期:2008年51-9]
- On page 1771, the author listed as "Anna Bottonocetti" should instead be "Anna Bottoncetti".
- Molecular Characterization of Macbecin as an Hsp90 Inhibitor.
[作者:Martin, Christine J.;Gaisser, Sabine;Challis, Iain R.;Carletti, Isabelle;Wilkinson, Barrie;Gregory, Matthew;Prodromou, Chrisostomos;Roe, S. Mark;Pearl, Laurence H.;Boyd, Susan M.;Zhang, Ming-Qiang;,期刊:Journal of Medicinal Chemistry, 页码:2853-2857 , 文章类型: 研究论文,,卷期:2008年51-9]
- Macbecin compares favorably to geldanamycin as an Hsp90 inhibitor, being more sol., stable, more potently inhibiting ATPase activity (IC50 = 2 mM) and binding with higher affinity (Kd = 0.24 mM). Structural studies reve...
- A Mutual Prodrug Ester of GABA and Perphenazine Exhibits Antischizophrenic Efficacy with Diminished Extrapyramidal Effects.
[作者:Nudelman, Abraham;Gil-Ad, Irit;Shpaisman, Nava;Terasenko, Igor;Ron, Hanna;Savitsky, Kinneret;Geffen, Yona;Weizman, Abraham;Rephaeli, Ada;,期刊:Journal of Medicinal Chemistry, 页码:2858-2862 , 文章类型: 研究论文,,卷期:2008年51-9]
- The perphenazine and fluphenazine GABA esters 3 and 4 evaluated in rat models for antipsychotic activity displayed a significant decrease of catalepsy assocd. with increased prolactin blood levels. Efficacy was evaluate...
- Synthesis of Indoleamine 2,3-Dioxygenase Inhibitory Analogues of the Sponge Alkaloid Exiguamine A.
[作者:Carr, Gavin;Chung, Marco K. W.;Mauk, A. Grant;Andersen, Raymond J.;,期刊:Journal of Medicinal Chemistry, 页码:2634-2637 , 文章类型: 研究论文,,卷期:2008年51-9]
- Synthetic analogs (e.g. I) of the sponge natural product exiguamine A have been prepd. and evaluated for their ability to inhibit indoleamine 2,3-dioxygenase in vitro.
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