- Effect of Fluorination on the Pharmacological Profile of 11b Isomers of Fulvestrant in Breast Carcinoma Cells.
[作者：Agouridas, Vangelis;Magnier, Emmanuel;Blazejewski, Jean-Claude;Laios, Ioanna;Cleeren, Anny;Nonclercq, Denis;Laurent, Guy;Leclercq, Guy;,期刊：Journal of Medicinal Chemistry, 页码：883-887 , 文章类型： 研究论文，,卷期：2009年52-3]
- We describe the synthesis of an 11b isomer 3 of the steroidal antiestrogen fulvestrant 2. Partial fluorination of the 11b side chain in 3 leads to 4, which still shows strong antiproliferative activity on MCF-7 cells. ...
- Structure-Activity Relationship and Studies on the Molecular Mechanism of Leishmanicidal N,C-Coupled Arylisoquinolinium Salts.
[作者：Ponte-Sucre, Alicia;Gulder, Tanja;Wegehaupt, Annemarie;Albert, Christoph;Rikanovic, Carina;Schaeflein, Leonhard;Frank, Andreas;Schultheis, Martina;Unger, Matthias;Holzgrabe, Ulrike;Bringmann, Gerhard;Moll, Heidrun;,期刊：Journal of Medicinal Chemistry, 页码：626-636 , 文章类型： 研究论文，,卷期：2009年52-3]
- Alternative drugs against leishmaniasis are desperately needed. Antimonials, the main chemotherapeutic tool, cause serious side effects and promote chemoresistance. We previously demonstrated that representatives of N,C...
- Synthesis, Reduction Potentials, and Antitubercular Activity of Ring A/B Analogues of the Bioreductive Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[ 2,1-b][1,3]oxazine (PA-824).
[作者：Thompson, Andrew M.;Blaser, Adrian;Anderson, Robert F.;Shinde, Sujata S.;Franzblau, Scott G.;Ma, Zhenkun;Denny, William A.;Palmer, Brian D.;,期刊：Journal of Medicinal Chemistry, 页码：637-645 , 文章类型： 研究论文，,卷期：2009年52-3]
- The nitroimidazooxazine I (PA-824) is a new class of bioreductive drug for tuberculosis. A series of related bicyclic nitroheterocycles was synthesized, designed to have a wide range of one-electron redn. potentials E(1...
- Cloning, Expression, Post-Translational Modifications and Inhibition Studies on the Latest Mammalian Carbonic Anhydrase Isoform, CA XV.
[作者：Hilvo, Mika;Salzano, Anna Maria;Innocenti, Alessio;Kulomaa, Markku S.;Scozzafava, Andrea;Scaloni, Andrea;Parkkila, Seppo;Supuran, Claudiu T.;,期刊：Journal of Medicinal Chemistry, 页码：646-654 , 文章类型： 研究论文，,卷期：2009年52-3]
- We have cloned and purified to homogeneity the latest member of the mammalian a-carbonic anhydrase (CA, EC 4.2.1.1) family, the mouse CA XV (mCA XV) protein. An investigation on the post-translational modifications of t...
- 2-[(2,3-Dihydro-1H-indol-1-yl)methyl]melatonin Analogues: A Novel Class of MT2-Selective Melatonin Receptor Antagonists.
[作者：Zlotos, Darius P.;Attia, Mohamed I.;Julius, Justin;Sethi, Shalini;Witt-Enderby, Paula A.;,期刊：Journal of Medicinal Chemistry, 页码：826-833 , 文章类型： 研究论文，,卷期：2009年52-3]
- A novel series of 2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogs I [R = Me, R' = Me, propyl; R = H, R' = Me, Et, cyclobutyl] and II [X = 5-methoxyindolin-1-yl, 5-methylindolin-1-yl, 5-bromoindolin-1-yl, pyrrolidi...
- Discovery of Chiral Cyclopropyl Dihydro-Alkylthio-Benzyl-Oxopyrimidine (S-DABO) Derivatives as Potent HIV-1 Reverse Transcriptase Inhibitors with High Activity Against Clinically Relevant Mutants.
[作者：Radi, Marco;Maga, Giovanni;Alongi, Maddalena;Angeli, Lucilla;Samuele, Alberta;Zanoli, Samantha;Bellucci, Luca;Tafi, Andrea;Casaluce, Gianni;Giorgi, Gianluca;Armand-Ugon, Mercedes;Gonzalez, Emmanuel;Este, Jose A.;Baltzinger, Mireille;Bec, Guillaume;Dumas,,期刊：Journal of Medicinal Chemistry, 页码：840-851 , 文章类型： 研究论文，,卷期：2009年52-3]
- The role played by stereochem. in the C2-substituent (left part) on the S-DABO scaffold for anti-HIV-1 activity has been investigated for the first time. A series of S-DABO analogs, where the double bond in the C2-subst...
- N,N-bis(Cyclohexanol)amine Aryl Esters: A New Class of Highly Potent Transporter-Dependent Multidrug Resistance Inhibitors.
[作者：Martelli, Cecilia;Alderighi, Daniela;Coronnello, Marcella;Dei, Silvia;Frosini, Maria;Le Bozec, Benedicte;Manetti, Dina;Neri, Annalisa;Romanelli, Maria Novella;Salerno, Milena;Scapecchi, Serena;Mini, Enrico;Sgaragli, Giampietro;Teodori, Elisabetta;,期刊：Journal of Medicinal Chemistry, 页码：807-817 , 文章类型： 研究论文，,卷期：2009年52-3]
- A new series of Pgp-dependent MDR inhibitors having a N,N-bis(cyclohexanol)amine scaffold was designed on the basis of the frozen analog approach. The scaffold chosen gives origin to different geometrical isomers. The ...
- The Discovery of a Selective, Small Molecule Agonist for the Mas-Related Gene X1 Receptor.
[作者：Wroblowski, Berthold;Wigglesworth, Mark J.;Szekeres, Philip G.;Smith, Graham D.;Rahman, Shahzad S.;Nicholson, Neville H.;Muir, Alison I.;Hall, Adrian;Heer, Jag P.;Garland, Stephen L.;Coates, William J.;,期刊：Journal of Medicinal Chemistry, 页码：818-825 , 文章类型： 研究论文，,卷期：2009年52-3]
- The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small mo...
- Novel Heteroaromatic Organofluorine Inhibitors of Fructose-1,6-bisphosphatase.
[作者：Rudnitskaya, Aleksandra;Huynh, Ken;Torok, Bela;Stieglitz, Kimberly;,期刊：Journal of Medicinal Chemistry, 页码：878-882 , 文章类型： 研究论文，,卷期：2009年52-3]
- A broad group of compds. including substituted pyrazoles, pyrroles, indoles, and carbazoles were screened to identify potential inhibitor lead compds. of fructose-1,6-bisphosphatase (FBPase). Best inhibitors are (1H-ind...
- N-[6-Amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A Receptor Antagonists with Improved Drug Like Properties and in Vivo Efficacy.
[作者：Lanier, Marion C.;Moorjani, Manisha;Luo, Zhiyong;Chen, Yongsheng;Lin, Emily;Tellew, John E.;Zhang, Xiaohu;Williams, John P.;Gross, Raymond S.;Lechner, Sandra M.;Markison, Stacy;Joswig, Tanya;Kargo, William;Piercey, Jaime;Santos, Mark;Malany, Siobhan;Zhao,,期刊：Journal of Medicinal Chemistry, 页码：709-717 , 文章类型： 研究论文，,卷期：2009年52-3]
- In the present article, we report on a strategy to improve the phys. properties of a series of small mol. human adenosine 2A (hA2A) antagonists. One of the arom. rings typical of this series of antagonists is replaced w...
- Additivity in the Analysis and Design of HIV Protease Inhibitors.
[作者：Jorissen, Robert N.;Reddy, G. S. Kiran Kumar;Ali, Akbar;Altman, Michael D.;Chellappan, Sripriya;Anjum, Saima G.;Tidor, Bruce;Schiffer, Celia A.;Rana, Tariq M.;Gilson, Michael K.;,期刊：Journal of Medicinal Chemistry, 页码：737-754 , 文章类型： 研究论文，,卷期：2009年52-3]
- We explore the applicability of an additive treatment of substituent effects to the anal. and design of HIV protease inhibitors. Affinity data for a set of inhibitors with a common chem. framework were analyzed to provi...
- Guanidine and 2-Aminoimidazoline Aromatic Derivatives as a2-Adrenoceptor Ligands: Searching for Structure-Activity Relationships.
[作者：Rodriguez, Fernando;Rozas, Isabel;Ortega, Jorge E.;Erdozain, Amaia M.;Meana, J. Javier;Callado, Luis F.;,期刊：Journal of Medicinal Chemistry, 页码：601-609 , 文章类型： 研究论文，,卷期：2009年52-3]
- In this paper, we report the synthesis of three new 2-aminoimidazoline (compds. 4b, 5b, and 6b) and three new guanidine derivs. (compds. 7b, 8b, and 9b) as potential a2-adrenoceptor antagonists for the treatment of depre...
- Novel Non-Peptide Nociceptin/Orphanin FQ Receptor Agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzim idazole: Design, Synthesis, and Structure-Activity Relationship of Oral Receptor Occupancy in the Brain for Orally Potent
[作者：Hayashi, Shigeo;Hirao, Akiko;Imai, Aki;Nakamura, Hiroshi;Murata, Yoshinori;Ohashi, Katsuyo;Nakata, Eriko;,期刊：Journal of Medicinal Chemistry, 页码：610-625 , 文章类型： 研究论文，,卷期：2009年52-3]
- An endogenous heptadecapeptide, nociceptin/orphanin FQ (N/OFQ), and a G-protein-coupled receptor, N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor], have been described in terms of its structure, d...
- Structures of Falcipain-2 and Falcipain-3 Bound to Small Molecule Inhibitors: Implications for Substrate Specificity.
[作者：Kerr, Iain D.;Lee, Ji H.;Pandey, Kailash C.;Harrison, Amanda;Sajid, Mohammed;Rosenthal, Philip J.;Brinen, Linda S.;,期刊：Journal of Medicinal Chemistry, 页码：852-857 , 文章类型： 研究论文，,卷期：2009年52-3]
- Falcipain-2 and falcipain-3 are crit. hemoglobinases of Plasmodium falciparum, the most virulent human malaria parasite. We have detd. the 2.9 ?crystal structure of falcipain-2 in complex with the epoxysuccinate E64 and...
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