- Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
[作者：Minarini, Anna;Marucci, Gabriella;Bellucci, Cristina;Giorgi, Gianluca;Tumiatti, Vincenzo;Bolognesi, Maria Laura;Matera, Riccardo;Rosini, Michela;Melchiorre, Carlo;,期刊：Bioorganic & Medicinal Chemistry, 页码：7311-7320 , 文章类型： 研究论文，,卷期：2008年16-15]
- Pirenzepine (2) is one of the most selective muscarinic M1 vs. M2 receptor antagonists known. A series of 2 analogs, in which the piperazyl moiety was replaced by a cis- and trans-cyclohexane-1,2-diamine (3-6) or a tran...
- Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
[作者：Ablordeppey, Seth Y.;Altundas, Ramazan;Bricker, Barbara;Zhu, Xue Y.;Kumar, Eyunni V. K. Suresh;Jackson, Tanise;Khan, Abdul;Roth, Bryan L.;,期刊：Bioorganic & Medicinal Chemistry, 页码：7291-7301 , 文章类型： 研究论文，,卷期：2008年16-15]
- The synthesis and exploration of novel butyrophenones have led to the identification of a diazepane analog of haloperidol, 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one (compd. 13) with an intere...
- Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: Synthesis, SAR analysis, and biological activity.
[作者：Zhang, Shixuan;Ma, Jigang;Bao, Yongming;Yang, Puwen;Zou, Liang;Li, Kangjian;Sun, Xiaodan;,期刊：Bioorganic & Medicinal Chemistry, 页码：7128-7133 , 文章类型： 研究论文，,卷期：2008年16-15]
- A series of nitrogen-contg. flavonoid analogs were designed and synthesized by Mannich reaction, and screened for the inhibitory activities of cyclin-dependent kinases using a FRET-based biochem. assay method. The resul...
- Design and synthesis of novel oxazole containing 1,3-Dioxane-2-carboxylic acid derivatives as PPAR a/g dual agonists.
[作者：Pingali, Harikishore;Jain, Mukul;Shah, Shailesh;Makadia, Pankaj;Zaware, Pandurang;Goel, Ashish;Patel, Megha;Giri, Suresh;Patel, Harilal;Patel, Pankaj;,期刊：Bioorganic & Medicinal Chemistry, 页码：7117-7127 , 文章类型： 研究论文，,卷期：2008年16-15]
- A few novel 1,3-dioxane carboxylic acid derivs. were designed and synthesized to aid in the characterization of PPAR a/g dual agonists. Structural requirements for PPARa/g dual agonism of 1,3-dioxane carboxylic acid deri...
- Synthesis and antiviral evaluation of some new pyrazole and fused pyrazolopyrimidine derivatives.
[作者：Rashad, Aymn E.;Hegab, Mohamed I.;Abdel-Megeid, Randa E.;Micky, Jehan A.;Abdel-Megeid, Farouk M. E.;,期刊：Bioorganic & Medicinal Chemistry, 页码：7102-7106 , 文章类型： 研究论文，,卷期：2008年16-15]
- 2, 4, 8, and 9 were synthesized. Also, some acyclic S-nucleosides of pyrazolo[3,4-d]pyrimidine derivs. 10-13 were prepd. via reaction of pyrazolo[3,4-d]pyrimidine-4(3H)-thione deriv. 9 with some acyclic sugars. Moreove...
- Sulfur-substituted naphthalimides as photoactivatable anticancer agents: DNA interaction, fluorescence imaging, and phototoxic effects in cultured tumor cells.
[作者：Ott, Ingo;Xu, Yufang;Liu, Jianwen;Kokoschka, Malte;Harlos, Melanie;Sheldrick, William S.;Qian, Xuhong;,期刊：Bioorganic & Medicinal Chemistry, 页码：7107-7116 , 文章类型： 研究论文，,卷期：2008年16-15]
- A series of sulfur-substituted naphthalimides (1-5) was prepd. and investigated as antitumor drugs. Initial DNA interaction studies (by the fluorescence quenching method, UV/vis and CD spectroscopy, thermal denaturation...
- Characterization of the PON1 active site using modeling simulation, in relation to PON1 lactonase activity.
[作者：Tavori, Hagai;Khatib, Soliman;Aviram, Michael;Vaya, Jacob;,期刊：Bioorganic & Medicinal Chemistry, 页码：7504-7509 , 文章类型： 研究论文，,卷期：2008年16-15]
- Paraoxonase1 (PON1) is a HDL bound enzymem, and many of the anti-atherogenic properties of HDL are attributed to PON1. The enzyme precise mechanism of protective action and its endogenous substrate remain elusive. PON1...
- In vitro inhibition of glycogen-degrading enzymes and glycosidases by six-membered sugar mimics and their evaluation in cell cultures.
[作者：Kuriyama, Chinami;Kamiyama, Ogusa;Ikeda, Kyoko;Sanae, Fujiko;Kato, Atsushi;Adachi, Isao;Imahori, Tatsushi;Takahata, Hiroki;Okamoto, Tadashi;Asano, Naoki;,期刊：Bioorganic & Medicinal Chemistry, 页码：7330-7336 , 文章类型： 研究论文，,卷期：2008年16-15]
- We investigated in vitro inhibition of mammalian carbohydrate-degrading enzymes by six-membered sugar mimics and their evaluation in cell cultures. 1-Deoxynojirimycin (DNJ) showed no significant inhibition toward glycoge...
- Illudalic acid as a potential LAR inhibitor: Synthesis, SAR, and preliminary studies on the mechanism of action.
[作者：Ling, Qing;Huang, Yue;Zhou, Yueyang;Cai, Zhengliang;Xiong, Bing;Zhang, Yahui;Ma, Lanping;Wang, Xin;Li, Xin;Li, Jia;Shen, Jingkang;,期刊：Bioorganic & Medicinal Chemistry, 页码：7399-7409 , 文章类型： 研究论文，,卷期：2008年16-15]
- A novel synthesis of the human leukocyte common antigen-related (LAR) phosphatase inhibitor, illudalic acid, has been achieved by a route more amenable to structure modifications. A series of simpler analogs of illudali...
- Phenyl phosphotriester derivatives of AZT: Variations upon the SATE moiety.
[作者：Villard, Anne-Laure;Coussot, Gaelle;Lefebvre, Isabelle;Augustijns, Patrick;Aubertin, Anne-Marie;Gosselin, Gilles;Peyrottes, Suzanne;Perigaud, Christian;,期刊：Bioorganic & Medicinal Chemistry, 页码：7321-7329 , 文章类型： 研究论文，,卷期：2008年16-15]
- Synthesis, in vitro anti-HIV activity, stability studies as well as potential phosphotriester derivs. of AZT (zidovudine; 3'-azido-2',3'-dideoxythymidine) are described herein. These pronucleotides are characterized by ...
- Hanultarin, a cytotoxic lignan as an inhibitor of actin cytoskeleton polymerization from the seeds of Trichosanthes kirilowii.
[作者：Moon, Surk-Sik;Rahman, Aziz Abdur;Kim, Joo-Young;Kee, Sun-Ho;,期刊：Bioorganic & Medicinal Chemistry, 页码：7264-7269 , 文章类型： 研究论文，,卷期：2008年16-15]
- Bioactivity-directed fractionation of exts. from the seeds of Trichosanthes kirilowii led to the isolation of (-)-1-O-feruloylsecoisolariciresinol (2), named hanultarin, In addn., four known lignans were also isolated, i...
- Remarkable DNA binding affinity and potential anticancer activity of pyrrolo[2,1-c][1,4]benzodiazepine-naphthalimide conjugates linked through piperazine side-armed alkane spacers.
[作者：Kamal, Ahmed;Ramu, R.;Tekumalla, Venkatesh;Khanna, G. B. Ramesh;Barkume, Madan S.;Juvekar, Aarti S.;Zingde, Surekha M.;,期刊：Bioorganic & Medicinal Chemistry, 页码：7218-7224 , 文章类型： 研究论文，,卷期：2008年16-15]
- A series of pyrrolobenzodiazepine-naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high D...
- Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents.
[作者：Ty, Nancy;Dupeyre, Gregory;Chabot, Guy G.;Seguin, Johanne;Tillequin, Francois;Scherman, Daniel;Michel, Sylvie;Cachet, Xavier;,期刊：Bioorganic & Medicinal Chemistry, 页码：7494-7503 , 文章类型： 研究论文，,卷期：2008年16-15]
- 6-Methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075) (1) is a potent inhibitor of tubulin polymn. which exhibits both in vitro and in vivo activities against a broad spectrum of solid tumors. This compd. was de...
- QSAR prediction of inhibition of aldose reductase for flavonoids.
[作者：Mercader, Andrew G.;Duchowicz, Pablo R.;Fernandez, Francisco M.;Castro, Eduardo A.;Bennardi, Daniel O.;Autino, Juan C.;Romanelli, Gustavo P.;,期刊：Bioorganic & Medicinal Chemistry, 页码：7470-7476 , 文章类型： 研究论文，,卷期：2008年16-15]
- We performed a predictive anal. based on quant. structure-activity relationships (QSAR) of an important property of flavonoids, which is the inhibition (IC50) of aldose reductase (AR). The importance of AR inhibition is...
- Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: Inhibition of inosine monophosphate dehydrogenase.
[作者：Chen, Liqiang;Petrelli, Riccardo;Olesiak, Magdalena;Wilson, Daniel J.;Labello, Nicholas P.;Pankiewicz, Krzysztof W.;,期刊：Bioorganic & Medicinal Chemistry, 页码：7462-7469 , 文章类型： 研究论文，,卷期：2008年16-15]
- Synthesis of novel inhibitors of human IMP dehydrogenase is analogs 5-8 of earlier reported mycophenolic adenine methylenebis(phosphonate)s 1-3. The parent bis(phosphonate) 1 and its bis(sulfonamide) analog 5 showed sim...
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