- Comparative Positron-Emission Tomography (PET) Imaging and Phototherapeutic Potential of 124I- Labeled Methyl- 3-(1'-iodobenzyloxyethyl)pyropheophorbide-a vs the Corresponding Glucose and Galactose Conjugates.
[作者：Pandey, Suresh K.;Sajjad, Munawwar;Chen, Yihui;Zheng, Xiang;Yao, Rutao;Missert, Joseph R.;Batt, Carrie;Nabi, Hani A.;Oseroff, Allan R.;Pandey, Ravindra K.;,期刊：Journal of Medicinal Chemistry, 页码：445-455 , 文章类型： 研究论文，,卷期：2009年52-2]
- In our present study, 3-(1'-m-iodobenzyloxyethyl)pyropheophorbide-a Me ester 1, 3-(1'-m-iodobenzyloxyethyl)-172-{(2-deoxy)glucose}pyropheophorbide- a 2, and 3-(1'-m-iodobenzyloxyethyl)-172-{(1-deoxy)galactose}pyropheopho...
- Mechanism of p300 Specific Histone Acetyltransferase Inhibition by Small Molecules.
[作者：Arif, M.;Pradhan, Suman Kalyan;R, Thanuja G.;Vedamurthy, B. M.;Agrawal, Shipra;Dasgupta, Dipak;Kundu, Tapas K.;,期刊：Journal of Medicinal Chemistry, 页码：267-277 , 文章类型： 研究论文，,卷期：2009年52-2]
- Dysfunction of histone acetyltransferases (HATs) leads to several diseases including cancer, diabetes, and asthma. Therefore, small mol. inhibitors and activators of HATs are being considered as new generation therapeut...
- A Novel Histone Acetyltransferase Inhibitor Modulating Gcn5 Network: Cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl]hydrazone.
[作者：Chimenti, Franco;Bizzarri, Bruna;Maccioni, Elias;Secci, Daniela;Bolasco, Adriana;Chimenti, Paola;Fioravanti, Rossella;Granese, Arianna;Carradori, Simone;Tosi, Federica;Ballario, Paola;Vernarecci, Stefano;Filetici, Patrizia;,期刊：Journal of Medicinal Chemistry, 页码：530-536 , 文章类型： 研究论文，,卷期：2009年52-2]
- Acetylation is a key modulator of genome accessibility through decondensation of the chromatin structure. The balance between acetylation and opposite deacetylation is, in fact, a prerequisite for several cell functions...
- Inhibition of MDR1 Activity in Vitro by a Novel Class of Diltiazem Analogues: Toward New Candidates.
[作者：Viale, Maurizio;Cordazzo, Cinzia;Cosimelli, Barbara;de Totero, Daniela;Castagnola, Patrizio;Aiello, Cinzia;Severi, Elda;Petrillo, Giovanni;Cianfriglia, Maurizio;Spinelli, Domenico;,期刊：Journal of Medicinal Chemistry, 页码：259-266 , 文章类型： 研究论文，,卷期：2009年52-2]
- The reversal of multidrug resistance by 22 mols. [8-aryl-8-hydroxy-5-R'-8H-[1,4]thiazino[3,4-c][1,2,4]oxadiazol-3-ones (1a-i) and 8-aryl-8-alkoxy-5-methyl-8H-[1,4]thiazino[3,4-c][1,2,4]oxadiazol-3-ones (2a-m)] related to...
- Non-Peptide Macrocyclic Histone Deacetylase Inhibitors.
[作者：Oyelere, Adegboyega K.;Chen, Po C.;Guerrant, William;Mwakwari, Sandra C.;Hood, Rebecca;Zhang, Yunzhe;Fan, Yuhong;,期刊：Journal of Medicinal Chemistry, 页码：456-468 , 文章类型： 研究论文，,卷期：2009年52-2]
- Inhibition of histone deacetylase inhibitors (HDACi) hold great promise in cancer therapy because of their demonstrated ability to arrest proliferation of nearly all transformed cell types. Of the several structurally d...
- Design, Structure-Activity Relationships and in Vivo Characterization of 4-Amino-3-benzimidazol-2-ylhydroquinolin-2-ones: A Novel Class of Receptor Tyrosine Kinase Inhibitors.
[作者：Renhowe, Paul A.;Pecchi, Sabina;Shafer, Cynthia M.;Machajewski, Timothy D.;Jazan, Elisa M.;Taylor, Clarke;Antonios-McCrea, William;McBride, Christopher M.;Frazier, Kelly;Wiesmann, Marion;Lapointe, Gena R.;Feucht, Paul H.;Warne, Robert L.;Heise, Carla C.;M,期刊：Journal of Medicinal Chemistry, 页码：278-292 , 文章类型： 研究论文，,卷期：2009年52-2]
- The inhibition of key receptor tyrosine kinases (RTKs) that are implicated in tumor vasculature formation and maintenance, as well as tumor progression and metastasis, has been a major focus in oncol. research over the l...
- Four-Dimensional Docking: A Fast and Accurate Account of Discrete Receptor Flexibility in Ligand Docking.
[作者：Bottegoni, Giovanni;Kufareva, Irina;Totrov, Maxim;Abagyan, Ruben;,期刊：Journal of Medicinal Chemistry, 页码：397-406 , 文章类型： 研究论文，,卷期：2009年52-2]
- Many available methods aimed at incorporating the receptor flexibility in ligand docking are computationally expensive, require a high level of user intervention, and were tested only on benchmarks of limited size and di...
- Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopip eridine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist.
[作者：Griffith, David A.;Hadcock, John R.;Black, Shawn C.;Iredale, Philip A.;Carpino, Philip A.;DaSilva-Jardine, Paul;Day, Robert;DiBrino, Joseph;Dow, Robert L.;Landis, Margaret S.;O'Connor, Rebecca E.;Scott, Dennis O.;,期刊：Journal of Medicinal Chemistry, 页码：234-237 , 文章类型： 研究论文，,卷期：2009年52-2]
- We report the structure-activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compd. 3a (I) showed subnanomolar potency at human CB1 receptors in bindin...
- First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery.
[作者：Menichincheri, Maria;Bargiotti, Alberto;Berthelsen, Jens;Bertrand, Jay A.;Bossi, Roberto;Ciavolella, Antonella;Cirla, Alessandra;Cristiani, Cinzia;Croci, Valter;D'Alessio, Roberto;Fasolini, Marina;Fiorentini, Francesco;Forte, Barbara;Isacchi, Antonella;Ma,期刊：Journal of Medicinal Chemistry, 页码：293-307 , 文章类型： 研究论文，,卷期：2009年52-2]
- Cdc7 kinase is a key regulator of the S-phase of the cell cycle, known to promote the activation of DNA replication origins in eukaryotic organisms. Cdc7 inhibition can cause tumor-cell death in a p53-independent manner...
- Carbonic Anhydrase Inhibitors. Comparison of Chlorthalidone and Indapamide X-ray Crystal Structures in Adducts with Isozyme II: When Three Water Molecules and the Keto-Enol Tautomerism Make the Difference.
[作者：Temperini, Claudia;Cecchi, Alessandro;Scozzafava, Andrea;Supuran, Claudiu T.;,期刊：Journal of Medicinal Chemistry, 页码：322-328 , 文章类型： 研究论文，,卷期：2009年52-2]
- Thiazide diuretics inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a different profile as compared to classical inhibitors. Acting as moderate-weak inhibitors of CA II and CA I, chlorthalidone...
- Dual Integrin and Gastrin-Releasing Peptide Receptor Targeted Tumor Imaging Using 18F-labeled PEGylated RGD-Bombesin Heterodimer 18F-FB-PEG3-Glu-RGD-BBN.
[作者：Liu, Zhaofei;Yan, Yongjun;Chin, Frederic T.;Wang, Fan;Chen, Xiaoyuan;,期刊：Journal of Medicinal Chemistry, 页码：425-432 , 文章类型： 研究论文，,卷期：2009年52-2]
- Radiolabeled RGD and bombesin peptides have been extensively investigated for tumor integrin avb3 and GRPR imaging, resp. Due to the fact that many tumors are both integrin and GRPR pos., we designed and synthesized a h...
- Multivalent Scaffolds for Affinity Maturation of Small Molecule Cell Surface Binders and Their Application to Prostate Tumor Targeting.
[作者：Humblet, Valerie;Misra, Preeti;Bhushan, Kumar R.;Nasr, Khaled;Ko, Yao-Sen;Tsukamoto, Takashi;Pannier, Nadine;Frangioni, John V.;Maison, Wolfgang;,期刊：Journal of Medicinal Chemistry, 页码：544-550 , 文章类型： 研究论文，,卷期：2009年52-2]
- Adamantane scaffolds for affinity maturation of prostate cancer specific ligands of low mol. mass are described. These scaffolds are modular and can be used for conjugation of up to three ligands and an addnl. effector ...
- Structural Analysis of ARC-Type Inhibitor (ARC-1034) Binding to Protein Kinase A Catalytic Subunit and Rational Design of Bisubstrate Analogue Inhibitors of Basophilic Protein Kinases.
[作者：Lavogina, Darja;Lust, Marje;Viil, Indrek;Konig, Norbert;Raidaru, Gerda;Rogozina, Jevgenia;Enkvist, Erki;Uri, Asko;Bossemeyer, Dirk;,期刊：Journal of Medicinal Chemistry, 页码：308-321 , 文章类型： 研究论文，,卷期：2009年52-2]
- The crystal structure of a complex of the catalytic subunit (type a) of cAMP-dependent protein kinase (PKA Ca) with ARC-type inhibitor (ARC-1034), the presumed lead scaffold of previously reported adenosine-oligo-arginin...
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