- Evaluation of Radiolabeled (Hetero)Aromatic Analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for Imaging and Targeted Radionuclide Therapy of Melanoma.
[作者:Chezal, Jean-Michel;Papon, Janine;Labarre, Pierre;Lartigue, Claire;Galmier, Marie-Josephe;Decombat, Caroline;Chavignon, Olivier;Maublant, Jean;Teulade, Jean-Claude;Madelmont, Jean-Claude;Moins, Nicole;,期刊:Journal of Medicinal Chemistry, 页码:3133-3144 , 文章类型: 研究论文,,卷期:2008年51-11]
- Targeted radionuclide therapy using radioiodinated compds. with a specific affinity for melanoma tissue is a promising treatment for disseminated melanoma, but the candidate with the ideal kinetic profile remains to be d...
- Novel Inhibitors of the v-raf Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) Based on a 2,6-Disubstituted Pyrazine Scaffold.
[作者:Niculescu-Duvaz, Ion;Roman, Esteban;Whittaker, Steven R.;Friedlos, Frank;Kirk, Ruth;Scanlon, Ian J.;Davies, Lawrence C.;Niculescu-Duvaz, Dan;Marais, Richard;Springer, Caroline J.;,期刊:Journal of Medicinal Chemistry, 页码:3261-3274 , 文章类型: 研究论文,,卷期:2008年51-11]
- BRAF, a serine/threonine kinase, plays a key role in the development of certain types of cancer, particularly melanoma. 2-(3,4,5-Trimethoxyphenylamino)-6-(3-acetamidophenyl)pyrazine [I (R = BRAF inhibitor from a high-thr...
- Synthesis and Evaluation of [2-(4-Quinolyloxy)phenyl]methanone Derivatives: Novel Selective Inhibitors of Transforming Growth Factor-b Kinase.
[作者:Shimizu, Toshiyuki;Kimura, Kaname;Sakai, Teruyuki;Kawakami, Kazuki;Miyazaki, Tetsuko;Nakouji, Masayoshi;Ogawa, Akira;Ohuchi, Hitomi;Shimizu, Kiyoshi;,期刊:Journal of Medicinal Chemistry, 页码:3326-3329 , 文章类型: 研究论文,,卷期:2008年51-11]
- We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivs., e.g. I (R = Ph, R1 = H, Me, Br, MeO; R = Me, R1 = H, F, Me, MeO). These compds. had novel chem. structures that were distinct from those o...
- Antitumor agents 260. New desmosdumotin B analogues with improved in vitro anticancer activity.
[作者:Nakagawa-Goto, Kyoko;Bastow, Kenneth F.;Chen, Tzu-Hsuan;Morris-Natschke, Susan L.;Lee, Kuo-Hsiung;,期刊:Journal of Medicinal Chemistry, 页码:3297-3303 , 文章类型: 研究论文,,卷期:2008年51-11]
- Sixteen analogs of the unique flavonoid desmosdumotin B were prepd. and evaluated as in vitro inhibitors of the human KB cancer cell line and its MDR subclone, KB-VIN. 6,8,8-Tri-Et analogs showed enhanced showed signifi...
- Trifluoromethoxyl Substituted Phenylethylene Diamines as High Affinity s Receptor Ligands with Potent Anti-Cocaine Actions.
[作者:Smith, Trudy A.;Yang, Xiaowen;Wu, Huifang;Pouw, Buddy;Matsumoto, Rae R.;Coop, Andrew;,期刊:Journal of Medicinal Chemistry, 页码:3322-3325 , 文章类型: 研究论文,,卷期:2008年51-11]
- The phenylethylene diamines are a class of s receptor ligands with excellent selectivity over other biol. systems and with anti-cocaine actions that involve antagonism of s1 receptors. In order to increase the potency o...
- Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
[作者:Pedersen, Jenny M.;Matsson, Paer;Bergstroem, Christel A. S.;Norinder, Ulf;Hoogstraate, Janet;Artursson, Per;,期刊:Journal of Medicinal Chemistry, 页码:3275-3287 , 文章类型: 研究论文,,卷期:2008年51-11]
- The chem. space of registered oral drugs was explored for inhibitors of the human multidrug-resistance assocd. protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and drug-like compds. The data se...
- Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity.
[作者:Chackalamannil, Samuel;Wang, Yuguang;Greenlee, William J.;Hu, Zhiyong;Xia, Yan;Ahn, Ho-Sam;Boykow, George;Hsieh, Yunsheng;Palamanda, Jairam;Agans-Fantuzzi, Jacqueline;Kurowski, Stan;Graziano, Michael;Chintala, Madhu;,期刊:Journal of Medicinal Chemistry, 页码:3061-3064 , 文章类型: 研究论文,,卷期:2008年51-11]
- The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of this series has led to the discovery of 4 (SCH 530348), a pot...
- Lavendamycin Antitumor Agents: Structure-Based Design, Synthesis, and NAD(P)H:Quinone Oxidoreductase 1 (NQO1) Model Validation with Molecular Docking and Biological Studies.
[作者:Hassani, Mary;Cai, Wen;Koelsch, Katherine H.;Holley, David C.;Rose, Anthony S.;Olang, Fatemeh;Lineswala, Jayana P.;Holloway, William G.;Gerdes, John M.;Behforouz, Mohammad;Beall, Howard D.;,期刊:Journal of Medicinal Chemistry, 页码:3104-3115 , 文章类型: 研究论文,,卷期:2008年51-11]
- A 1H69 crystal structure-based in silico model of the NAD(P)H:quinone oxidoreductase 1 (NQO1) active site has been developed to facilitate NQO1-directed lavendamycin antitumor agent development. Lavendamycin analogs, e.g...
- Synthesis and Antibacterial Activity of Novel Pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic Acid Derivatives Carrying the 3-Cyclopropylaminomethyl-4-substituted-1-pyrrolidinyl Group as a C-10 Substituent.
[作者:Asahina, Yoshikazu;Takei, Masaya;Kimura, Tetsuya;Fukuda, Yasumichi;,期刊:Journal of Medicinal Chemistry, 页码:3238-3249 , 文章类型: 研究论文,,卷期:2008年51-11]
- Novel pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid derivs. I (R1 = Me, CH2F; R2, R3 = H, Me, F) carrying a 3-cyclopropylaminomethyl-4-substituted-1-pyrrolidinyl moiety at the C-10 position were synthesized and thei...
- Guanidine and 2-Aminoimidazoline Aromatic Derivatives as a2-Adrenoceptor Antagonists. 2. Exploring Alkyl Linkers for New Antidepressants.
[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:3304-3312 , 文章类型: 研究论文,,卷期:2008年51-11]
- The prepn. of a no. of (bis)guanidine and (bis)2-aminoimidazoline derivs. as potential a2-adrenoceptor antagonists for the treatment of depression was presented. Human brain tissue was used to measure their affinity tow...
- Benzoylurea Derivatives as a Novel Class of Antimitotic Agents: Synthesis, Anticancer Activity, and Structure-Activity Relationships.
[作者:Song, Dan-Qing;Wang, Yan;Wu, Lian-Zong;Yang, Peng;Wang, Yue-Ming;Gao, Li-Mei;Li, Yan;Qu, Jing-Rong;Wang, Yong-Hong;Li, Ying-Hong;Du, Na-Na;Han, Yan-Xing;Zhang, Zhi-Ping;Jiang, Jian-Dong;,期刊:Journal of Medicinal Chemistry, 页码:3094-3103 , 文章类型: 研究论文,,卷期:2008年51-11]
- Forty-six new compds. I (R1 = H, 2-Me, 4-MeO, 6-Br, 5-COOMe, etc.; R2 = CH2Br, CH2Cl, CH2I, CHBrMe, CHClMe) and II (X = O, S) were synthesized as 3-haloacylamino benzoylurea analogs and their anticancer activity has been...
- Novel Substituted Aminoalkylguanidines as Potential Antihyperglycemic and Food Intake-Reducing Agents.
[作者:Tassoni, Emanuela;Giannessi, Fabio;Brunetti, Tiziana;Pessotto, Pompeo;Renzulli, Michela;Travagli, Massimiliano;Rajamaeki, Suvi;Prati, Samanta;Dottori, Secondo;Corelli, Federico;Cabri, Walter;Carminati, Paolo;Botta, Maurizio;,期刊:Journal of Medicinal Chemistry, 页码:3073-3076 , 文章类型: 研究论文,,卷期:2008年51-11]
- and derivs. in C57BL/KsJ db/db diabetic mice, following identification by random screening of R2NHC(:NH)NHR1.MeSO3H (R1 = prenyl, R2 = 6-aminohexyl; R1 = prenyl, R2 = 4-aminobutyl) as potential antihyperglycemics and/or ...
- Assessment of scaffold hopping efficiency by use of molecular interaction fingerprints.
[作者:Venhorst, Jennifer;Nunez, Sara;Terpstra, Jan Willem;Kruse, Chris G.;,期刊:Journal of Medicinal Chemistry, 页码:3222-3229 , 文章类型: 研究论文,,卷期:2008年51-11]
- A novel scoring algorithm based on mol. interaction fingerprints (IFPs) was comparatively evaluated in its scaffold hopping efficiency against four virtual screening stds. (GlideXP, Gold, ROCS, and a Bayesian classifier)...
- A Prodomain Peptide of Plasmodium falciparum Cysteine Protease (Falcipain-2) Inhibits Malaria Parasite Development.
[作者:Korde, Reshma;Bhardwaj, Ashima;Singh, Rita;Srivastava, Anand;Chauhan, Virander S.;Bhatnagar, Raj K.;Malhotra, Pawan;,期刊:Journal of Medicinal Chemistry, 页码:3116-3123 , 文章类型: 研究论文,,卷期:2008年51-11]
- falciparum, is a promising target for antimalarial chemotherapy. Designing inhibitors that are highly selective for falcipain-2 has been difficult because of broad specificity of different cysteine proteinases. Because p...
- Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII.
[作者:D'Ambrosio, Katia;Vitale, Rosa-Maria;Dogne, Jean-Michel;Masereel, Bernard;Innocenti, Alessio;Scozzafava, Andrea;De Simone, Giuseppina;Supuran, Claudiu T.;,期刊:Journal of Medicinal Chemistry, 页码:3230-3237 , 文章类型: 研究论文,,卷期:2008年51-11]
- 2-Substituted-5-nitro-benzenesulfonamides incorporating a large variety of secondary/tertiary amines were explored as inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), with the aim of designing bioreduct...
- Development and Experimental Validation of a Docking Strategy for the Generation of Kinase-Targeted Libraries.
[作者:Gozalbes, Rafael;Simon, Laurence;Froloff, Nicolas;Sartori, Eric;Monteils, Claude;Baudelle, Romuald;,期刊:Journal of Medicinal Chemistry, 页码:3124-3132 , 文章类型: 研究论文,,卷期:2008年51-11]
- A high-throughput docking strategy for the filtering of in silico compds. and the generation of kinase-targeted libraries is described. Systematic docking and scoring in three kinase crystal 3D structures of 123 structur...
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