- Evidences for complex formation between L-dabPNA and aegPNA
[作者:Roviello, GN; Musumeci, D; Bucci, EM; Castiglione, M; Cesarani, A; Pedone, C; Piccialli, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4757-4760 , 文章类型: Article,,卷期:2008年18-17]
- Continuing our research on the development of nucleopeptides as ODN analogs for biomedical and bioengineering applications, here we report the synthesis and the chemical - physical characterization of a homoadenine hexam...
- A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins
[作者:Leyers, S; Hacker, HG; Wiendlocha, J; Guetschow, M; Wiese, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4761-4763 , 文章类型: Article,,卷期:2008年18-17]
- We present a novel lead for inhibitors of multidrug resistance-associated proteins (MRPs). Compound 1 (4-[(5,6,7,8-tetrahydro-4-oxo-4H-[1]benzothieno[2,3-d][1,3]thiazin-2-yl) amino] benzoic acid) was about six times more...
- Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain
[作者:Biswas, K; Aya, T; Qian, WY; Peterkin, TAN; Chen, JJ; Human, J; Hungate, RW; Kumar, G; Arik, L; Lester-Zeiner, D; Biddlecome, G; Manning, BH; Sun, H; Dong, H; Huang, M; Loeloff, R; Johnson, EJ; Askew, BC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4764-4769 , 文章类型: Article,,卷期:2008年18-17]
- We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modi. cations of the aryl moiety led to compound 26, bo...
- Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
[作者:Ellsworth, BA; Meng, W; Patel, M; Girotra, RN; Wu, G; Sher, PM; Hagan, DL; Obermeier, MT; Humphreys, WG; Robertson, JG; Wang, AY; Han, SP; Waldron, TL; Morgan, NN; Whaley, JM; Washburn, WN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4770-4773 , 文章类型: Article,,卷期:2008年18-17]
- Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed exce...
- Synthesis of a C-glucosylated cyclopropylamide and evaluation as a glycogen phosphorylase inhibitor
[作者:Bertus, P; Szymoniak, J; Jeanneau, E; Docsa, T; Gergely, P; Praly, JP; Vidal, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4774-4778 , 文章类型: Article,,卷期:2008年18-17]
- The synthesis of carbohydrate-based glycogen phosphorylase inhibitors is attractive for potential applications in the treatment of type 2 diabetes. A titanium-mediated synthesis led to a benzoylated C-glucosylated cyclop...
- Synthesis of N-acridinyl-N '-alkylguanidines: Dramatic influence of amine to guanidine replacement on the physicochemical properties
[作者:Zeghida, W; Debray, J; Michel, C; Milet, A; Dumy, P; Demeunynck, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4779-4782 , 文章类型: Article,,卷期:2008年18-17]
- Transformation of aminoacridines into N-acridinyl-N'-alkylguanidines is described. The chosen procedure allows introduction of pendent substituents (exemplified by N,N-dimethylaminopropyl chain) into key acridinyl thiour...
- An osteoclast-targeting agent for imaging and therapy of bone metastasis
[作者:Liu, W; Hajibeigi, A; Lin, M; Rostollan, CL; Kovacs, Z; Oz, OK; Sun, XK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4789-4793 , 文章类型: Article,,卷期:2008年18-17]
- A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N',N '',N '',N'"-tetraacetic acid, DOTA) and an osteoclast-targeting moiety ( bisphosphonate) was designed and...
- Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer
[作者:Scott, DA; Aquila, BM; Bebernitz, GA; Cook, DJ; Dakin, LA; Deegan, TL; Hattersley, MM; Ioannidis, S; Lyne, PD; Omer, CA; Ye, MW; Zheng, XL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4794-4797 , 文章类型: Article,,卷期:2008年18-17]
- The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides is reported, along with the pharmacokinetic properties and in vivo activity ...
- Highly functionalized 7-azaindoles as selective PPAR gamma modulators
[作者:Debenham, SD; Chan, A; Lau, FW; Liu, WG; Wood, HB; Lemme, K; Colwell, L; Habulihaz, B; Akiyama, TE; Einstein, M; Doebber, TW; Sharma, N; Wang, CF; Wu, M; Berger, JP; Meinke, PT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4798-4801 , 文章类型: Article,,卷期:2008年18-17]
- A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPAR gamma modulators (SPPAR gamma Ms). Addition of substituents at the 6-position of the 7-a...
- Development of TNKase specific cleavable peptide linked radioimmunoconjugates for radioimmunotherapy
[作者:Natarajan, A; Kumaresan, PR; DeNardo, SJ; DeNardo, GL; Mirick, G; Lam, KS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4802-4805 , 文章类型: Article,,卷期:2008年18-17]
- Radioimmunotherapy (RIT) is a method for selectively delivering radionuclides to cancer cells, while reducing the radiation dose to normal tissues. However, because of slow clearance of MAbs, normal tissues also received...
- The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels
[作者:Yamamoto, T; Niwa, S; Ohno, S; Tokumasu, M; Masuzawa, Y; Nakanishi, C; Nakajo, A; Onishi, T; Koganei, H; Fujita, S; Takeda, T; Kito, M; Ono, Y; Saitou, Y; Takahara, A; Iwata, S; Shoji, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4813-4816 , 文章类型: Article,,卷期:2008年18-17]
- In order to find an injectable and selective N-type calcium channel blocker, we have performed the structure-activity relationship (SAR) study on the 2-, 5-, and 6-position of 1,4-dihydropyridine-3-carboxylate derivative...
- Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands
[作者:Marinkovic, D; Tucci, FC; Tran, JA; Fleck, BA; Wen, J; Chen, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4817-4822 , 文章类型: Article,,卷期:2008年18-17]
- A series of piperazinebenzylalcohols were prepared and studied to compare with their ketone and amine analogs as MC4R antagonists. Several benzylalcohols such as 14a and 14g displayed low nanomolar binding affinities (K-...
- Synthesis and evaluation of indolinyl- and indolylphenylacetylenes as PET imaging agents for beta-amyloid plaques
[作者:Qu, WC; Choi, SR; Hou, C; Zhuang, ZP; Oya, S; Zhang, W; Kung, MP; Manchandra, R; Skovronsky, DM; Kung, HF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4823-4827 , 文章类型: Article,,卷期:2008年18-17]
- Two new phenylacetylene derivatives, 5-((4-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)phenyl)ethynyl)indoline 8 and 5-((4-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)phenyl)ethynyl)-1H-indole 14, targeting beta-amyloid ( Ab) plaques ha...
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