- Potential antitumoral properties of a new copper complex with santonic acid.
[作者:Williams, Patricia A. M.;Zinczuk, Juan;Barrio, Daniel A.;Piro, Oscar E.;Nascimento, Otaciro R.;Etcheverry, Susana B.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4313-4322 , 文章类型: 研究论文,,卷期:2008年16-8]
- A new copper(II) complex of santonic acid [Cu2(sant)4(H2O)2]?12 H2O has been prepd. and characterized by electronic, vibrational, EPR spectral studies, and stability detns. in soln. The presence of two antiferromagnetic...
- Labeling, characterization, and in vivo localization of a new 90Y-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with 99mTc-DPD complex.
[作者:Djokic, Divna Dj.;Jankovic, Drina Lj.;Nikolic, Nadezda S.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4457-4465 , 文章类型: 研究论文,,卷期:2008年16-8]
- The goal of this investigation was to examine the possibilities for yttrium-90-labeling of the 2,3-dicarboxypropane-1,1-diphosphonic acid (DPD), which is currently labeled with technetium-99m and as a 99mTc-DPD clin. use...
- Formation of fluorine-18 labeled diaryl ureas-labeled VEGFR-2/PDGFR dual inhibitors as molecular imaging agents for angiogenesis.
[作者:Ilovich, O.;Jacobson, O.;Aviv, Y.;Litchi, A.;Chisin, R.;Mishani, E.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4242-4251 , 文章类型: 研究论文,,卷期:2008年16-8]
- Urea subunits are common components of various pharmaceuticals' core structure. Since in most cases the design and development of PET biomarkers is based on approved or potential drugs, there is a growing need for a gen...
- Synthesis and anti-HIV1 biological activity of novel 5''-ATSAO compounds.
[作者:Tomassi, Cyrille;Nguyen Van Nhien, Albert;Marco-Contelles, Jose;Balzarini, Jan;Pannecouque, Christophe;De Clercq, Erik;Postel, Denis;,期刊:Bioorganic & Medicinal Chemistry, 页码:4733-4741 , 文章类型: 研究论文,,卷期:2008年16-8]
- ring with a Ph group at 5'' position were prepd. Biol. evaluation showed that Ph group gives rise to a dramatical decrease of the inhibitory effect.
- Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
[作者:Sato, Shinichi;Tetsuhashi, Masashi;Sekine, Keiko;Miyachi, Hiroyuki;Naito, Mikihiko;Hashimoto, Yuichi;Aoyama, Hiroshi;,期刊:Bioorganic & Medicinal Chemistry, 页码:4685-4698 , 文章类型: 研究论文,,卷期:2008年16-8]
- degrdn. of cellular inhibitor of apoptosis protein 1 (cIAP1), were designed and synthesized. Structure-activity relationship studies indicated that abs. configuration, hydrophobicity at the a-position of the internal am...
- Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease.
[作者:Shao, Yi-Ming;Yang, Wen-Bin;Kuo, Tun-Hsun;Tsai, Keng-Chang;Lin, Chun-Hung;Yang, An-Suei;Liang, Po-Huang;Wong, Chi-Huey;,期刊:Bioorganic & Medicinal Chemistry, 页码:4652-4660 , 文章类型: 研究论文,,卷期:2008年16-8]
- A series of trifluoromethyl ketones as SARS-Co-V 3CL protease inhibitors was developed. The inhibitors were synthesized in four steps from com. available compds. Three different amino acids were explored in the P1-posi...
- Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers.
[作者:Kimball, F. Scott;Turunen, Brandon J.;Ellis, Keith C.;Himes, Richard H.;Georg, Gunda I.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4367-4377 , 文章类型: 研究论文,,卷期:2008年16-8]
- enantiomers of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one. A biol. assay utilizing the HCT-116 colon cancer cell line to det. the cytotoxicity of these analogs revealed that only the (R)-enantiom...
- Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanec arboxylic acid and its 6-heptyl ester, a potent mGluR2 antagonist.
[作者:Sakagami, Kazunari;Yasuhara, Akito;Chaki, Shigeyuki;Yoshikawa, Ryoko;Kawakita, Yasunori;Saito, Akio;Taguchi, Takeo;Nakazato, Atsuro;,期刊:Bioorganic & Medicinal Chemistry, 页码:4359-4366 , 文章类型: 研究论文,,卷期:2008年16-8]
- In this paper, we describe the synthesis of (+)-(1R *,2R *)-2-[(1S *)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropaneca rboxylic acid (+)-16a, a compd., i.e., fluorinated at the alpha position of the ca...
- Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein.
[作者:Jain, Hiteshkumar D.;Zhang, Chunchun;Zhou, Shuo;Zhou, Hao;Ma, Jun;Liu, Xiaoxiang;Liao, Xuebin;Deveau, Amy M.;Dieckhaus, Christine M.;Johnson, Michael A.;Smith, Kirsten S.;Macdonald, Timothy L.;Kakeya, Hideaki;Osada, Hiroyuki;Cook, James M.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4626-4651 , 文章类型: 研究论文,,卷期:2008年16-8]
- Tryprostatin A is an inhibitor of breast cancer resistance protein, consequently a series of structure-activity studies on the cell cycle inhibitory effects of tryprostatin A analogs as potential antitumor antimitotic ag...
- Proteasome inhibition by peptide-semicarbazones.
[作者:Leban, Johann;Blisse, Marcus;Krauss, Babett;Rath, Sandra;Baumgartner, Roland;Seifert, Markus H. J.;,期刊:Bioorganic & Medicinal Chemistry, 页码:4579-4588 , 文章类型: 研究论文,,卷期:2008年16-8]
- Peptide-semicarbazones derived from Z-Trp-Trp-Phe-aldehyde inhibit the chymotryptic activity of the human proteasome at nanomolar concns., but are less active in a NFkB reporter gene assay. Cyclic semicarbazones, in con...
- Co-existence of a-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
[作者:Dodo, Kosuke;Aoyama, Atsushi;Noguchi-Yachide, Tomomi;Makishima, Makoto;Miyachi, Hiroyuki;Hashimoto, Yuichi;,期刊:Bioorganic & Medicinal Chemistry, 页码:4272-4285 , 文章类型: 研究论文,,卷期:2008年16-8]
- oxysterol-activated nuclear receptors, were recently found to recognize glucose as a physiol. ligand. On this basis, the authors have already developed novel LXR antagonists based upon a-glucosidase inhibitors derived f...
- Synthesis of caged 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones: Evaluating the minimum structure for apoptosis induction by gambogic acid.
[作者:Kuemmerle, Jared;Jiang, Songchun;Tseng, Ben;Kasibhatla, Shailaja;Drewe, John;Cai, Sui Xiong;,期刊:Bioorganic & Medicinal Chemistry, 页码:4233-4241 , 文章类型: 研究论文,,卷期:2008年16-8]
- We have reported the discovery of gambogic acid (GA) as a potent apoptosis inducer and the identification of transferrin receptor as its mol. target. To understand the basic pharmacophore of GA for inducing apoptosis an...
- Novel azaphilones, kasanosins A and B, which are specific inhibitors of eukaryotic DNA polymerases b and l from Talaromyces sp.
[作者:Kimura, Takuma;Nishida, Masayuki;Kuramochi, Kouji;Sugawara, Fumio;Yoshida, Hiromi;Mizushina, Yoshiyuki;,期刊:Bioorganic & Medicinal Chemistry, 页码:4594-4599 , 文章类型: 研究论文,,卷期:2008年16-8]
- Kasanosins A (1) and B (2) are novel azaphilones isolated from cultures of Talaromyces sp. derived from seaweed, and their structures were detd. by spectroscopic analyses. These compds. selectively inhibited the activit...
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