- Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids: Synthesis, nitric oxide release studies and anti-inflammatory activities.
[作者:Abdellatif, Khaled R. A.;Chowdhury, Morshed Alam;Dong, Ying;Knaus, Edward E.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6528-6534 , 文章类型: 研究论文,,卷期:2008年16-13]
- A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs) wherein an O 2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate (11a-c) NO-donor moiety is attached directly to the carbox...
- Unsymmetric aryl-alkyl disulfide growth inhibitors of methicillin-resistant Staphylococcus aureus and Bacillus anthracis.
[作者:Turos, Edward;Revell, Kevin D.;Ramaraju, Praveen;Gergeres, Danielle A.;Greenhalgh, Kerriann;Young, Ashley;Sathyanarayan, Nalini;Dickey, Sonja;Lim, Daniel;Alhamadsheh, Mamoun M.;Reynolds, Kevin;,期刊:Bioorganic & Medicinal Chemistry, 页码:6501-6508 , 文章类型: 研究论文,,卷期:2008年16-13]
- This study describes the antibacterial properties of synthetically produced mixed aryl-alkyl disulfide compds. as a means to control the growth of Staphylococcus aureus and Bacillus anthracis. Some of these compds. exer...
- Synthesis and characterization of water-soluble free-base, zinc and copper porphyrin-oligonucleotide conjugates.
[作者:Mammana, Angela;Asakawa, Tomohiro;Bitsch-Jensen, Klaus;Wolfe, Amanda;Chaturantabut, Saireudee;Otani, Yuko;Li, Xiaoxu;Li, Zengmin;Nakanishi, Koji;Balaz, Milan;Ellestad, George A.;Berova, Nina;,期刊:Bioorganic & Medicinal Chemistry, 页码:6544-6551 , 文章类型: 研究论文,,卷期:2008年16-13]
- The synthesis and characterization of a series of water-sol. free-base, zinc, and copper porphyrin-oligonucleotide (ODN) conjugates are reported. A non-charged tetraarylporphyrin was directly attached to the 5'-position...
- Synthesis of 3',4'-epoxynoraristeromycin analogs for molecular labeling probe of S-adenosyl-L-homocysteine hydrolase.
[作者:Kojima, Hiroharu;Kozaki, Atsushi;Iwata, Masafumi;Ando, Takayuki;Kitade, Yukio;,期刊:Bioorganic & Medicinal Chemistry, 页码:6575-6579 , 文章类型: 研究论文,,卷期:2008年16-13]
- 3',4'-Epoxynoraristeromycin analogs were designed and synthesized. Their affinities with human and Plasmodium falciparum S-adenosyl-L-homo-cysteine hydrolase were investigated.
- Synthetic and pharmacological studies on new simplified analogues of the potent actin-targeting Jaspamide.
[作者:Terracciano, Stefania;Bruno, Ines;D'Amico, Elisabetta;Bifulco, Giuseppe;Zampella, Angela;Sepe, Valentina;Smith, Charles D.;Riccio, Raffaele;,期刊:Bioorganic & Medicinal Chemistry, 页码:6580-6588 , 文章类型: 研究论文,,卷期:2008年16-13]
- In the recent years, the authors studied the cyclodepsipeptide jaspamide 1, an interesting marine metabolite, as a potent inhibitor against breast and prostate cancer and as a consequence of its ability to disrupt actin ...
- 2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
[作者:Pelletier, Jeffrey C.;Chengalvala, Murty;Cottom, Josh;Feingold, Irene;Garrick, Lloyd;Green, Daniel;Hauze, Diane;Huselton, Christine;Jetter, James;Kao, Wenling;Kopf, Gregory S.;Lundquist, Joseph T.;Mann, Charles;Mehlmann, John;Rogers, John;Shanno, Linda;Wr,期刊:Bioorganic & Medicinal Chemistry, 页码:6617-6640 , 文章类型: 研究论文,,卷期:2008年16-13]
- (Heterocyclic Compounds (More Than One Hetero Atom)) Section 2-Phenyl-4-piperazinylbenzimidazoles were prepd. as small mol. GnRH antagonists with nanomolar potency in in vitro binding and functional assays, excellent bio...
- Cu(I)-Glutathione complex: A potential source of superoxide radicals generation.
[作者:Speisky, Hernan;Gomez, Maritza;Carrasco-Pozo, Catalina;Pastene, Edgar;Lopez-Alarcon, Camilo;Olea-Azar, Claudio;,期刊:Bioorganic & Medicinal Chemistry, 页码:6568-6574 , 文章类型: 研究论文,,卷期:2008年16-13]
- Cu2+ ions and GSH mols. interact swiftly to form the complex Cu(I)-glutathione. We investigated the potential capacity of such complex to reduce mol. oxygen. The addn. of SOD to a soln. contg. Cu(I)-glutathione led to ...
- Synthesis and antitumor activity evaluations of albumin-binding prodrugs of CC-1065 analog.
[作者:Wang, Yuqiang;Jiang, Jie;Jiang, Xiaojian;Cai, Shaohui;Han, Hai;Li, Lianfa;Tian, Zhiming;Jiang, Wei;Zhang, Zaijun;Xiao, Ying;Wright, Susan C.;Larrick, James W.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6552-6559 , 文章类型: 研究论文,,卷期:2008年16-13]
- An albumin-binding prodrug of the extremely potent CC-1065 analog, (+)-FDI-CBI, has been synthesized. This analog, (+)-FDI-CBIM, formed an albumin conjugate when added to human albumin in vitro. A greater amt. (>3-fold...
- Citral derived amides as potent bacterial NorA efflux pump inhibitors.
[作者:Thota, Niranjan;Koul, Surrinder;Reddy, Mallepally V.;Sangwan, Payare L.;Khan, Inshad A.;Kumar, Ashwani;Raja, Alsaba F.;Andotra, Samar S.;Qazi, Ghulam N.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6535-6543 , 文章类型: 研究论文,,卷期:2008年16-13]
- Monoterpene citral and citronellal have been used as starting material for the prepn. of 5,9-dimethyl-deca-2,4,8-trienoic acid amides and 9-formyl-5-methyl-deca-2,4,8-trienoic acid amides. The amides on bioevaluation as...
- [11C]Cyclopropyl-FLB 457: A PET radioligand for low densities of dopamine D 2 receptors.
[作者:Airaksinen, Anu J.;Nag, Sangram;Finnema, Sjoerd J.;Mukherjee, Jogeshwar;Chattopadhyay, Sankha;Gulyas, Balazs;Farde, Lars;Halldin, Christer;,期刊:Bioorganic & Medicinal Chemistry, 页码:6467-6473 , 文章类型: 研究论文,,卷期:2008年16-13]
- (S)-5-Bromo-N-[(1-cyclopropylmethyl-2-pyrrolidinyl)methyl]-2,3-dimetho xybenzamide (4) has pico-molar in vitro binding affinity to D2 receptor (Ki (D2) = 0.003 nM) with lower affinity to D 3 receptor (Ki (D3) = 0.22 nM)....
- Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp.
[作者:Nukoolkarn, Veena S.;Saen-oon, Suwipa;Rungrotmongkol, Thanyada;Hannongbua, Supot;Ingkaninan, Kornkanok;Suwanborirux, Khanit;,期刊:Bioorganic & Medicinal Chemistry, 页码:6560-6567 , 文章类型: 研究论文,,卷期:2008年16-13]
- Two pyridoacridine alkaloids, including a known petrosamine and a new 2-bromoamphimedine, were isolated from a Thai marine sponge Petrosia n. sp. The alkaloids were characterized on the basis of 1D and 2D NMR, MS, and I...
- Alstilobanines A-E, new indole alkaloids from Alstonia angustiloba.
[作者:Koyama, Koichiro;Hirasawa, Yusuke;Zaima, Kazumasa;Hoe, Teh Chin;Chan, Kit-Lam;Morita, Hiroshi;,期刊:Bioorganic & Medicinal Chemistry, 页码:6483-6488 , 文章类型: 研究论文,,卷期:2008年16-13]
- Five new alkaloids, alstilobanines A (1)-E (5) were isolated from Alstonia angustiloba (Apocynaceae) and their structures were detd. by MS and 2D NMR spectral anal. Alstilobanines A-E showed a moderate vasorelaxant acti...
- Multidrug resistance reverting activity and antitumor profile of new phenothiazine derivatives.
[作者:Bisi, Alessandra;Meli, Maria;Gobbi, Silvia;Rampa, Angela;Tolomeo, Manlio;Dusonchet, Luisa;,期刊:Bioorganic & Medicinal Chemistry, 页码:6474-6482 , 文章类型: 研究论文,,卷期:2008年16-13]
- A series of easily affordable phenothiazine derivs. bearing a rigid but-2-ynyl amino side chain were synthesized and tested to evaluate the MDR reverting activity and full antitumor profile. Some compds. endowed with re...
- In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
[作者:Moarbess, Georges;Deleuze-Masquefa, Carine;Bonnard, Vanessa;Gayraud-Paniagua, Stephanie;Vidal, Jean-Remi;Bressolle, Francoise;Pinguet, Frederic;Bonnet, Pierre-Antoine;,期刊:Bioorganic & Medicinal Chemistry, 页码:6601-6610 , 文章类型: 研究论文,,卷期:2008年16-13]
- imiquimod, were synthesized, and their in vitro cytotoxic and pharmacodynamic activities were evaluated. In vitro cytotoxicity studies were assessed against melanoma (A375, M4Be, RPMI-7591), colon (LS174T), breast (MCF7...
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