- Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents
[作者:Li, X; Lu, X; Xing, M; Yang, XH; Zhao, TT; Gong, HB; Zhu, HL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3589-3593 , 文章类型: Article,,卷期:2012年22-11]
- A series of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives have been designed, synthesized and evaluated for their potential antiproliferation activity and Aurora-A kinase inhibitory activity. Among all the compou...
- Utilization of [C-11]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)]phenyl[C-11]ure2;ido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors
[作者:Asakawa, C; Ogawa, M; Fujinaga, M; Kumata, K; Xie, L; Yamasaki, T; Yui, J; Fukumura, T; Zhang, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3594-3597 , 文章类型: Article,,卷期:2012年22-11]
- N-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide (2), an ureido-substituted derivative of glycyrrhetinic acid (1), has been reported to display potent inhibitory activity for proteasome and kinase, ...
- Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents
[作者:Zhang, H; Liu, J; Zhang, LY; Kong, LY; Yao, HQ; Sun, HB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3598-3602 , 文章类型: Article,,卷期:2012年22-11]
- Ticagrelor (1) is the first reversible P2Y12 receptor antagonist blocking adenine diphosphate (ADP)-induced platelet aggregation with rapid onset and offset of effects. In this study, synthesis of ticagrelor and its deri...
- Synthesis and antimycobacterial activity of prodrugs of sulfur dioxide (SO2)
[作者:Malwal, SR; Sriram, D; Yogeeswari, P; Chakrapani, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3603-3606 , 文章类型: Article,,卷期:2012年22-11]
- Here, we synthesized and studied a library of 2,4-dinitrophenylsulfonamides that closely resembled N-benzyl-2,4-dinitrophenylsulfonamide (1), a thiol-activated prodrug of sulfur dioxide (SO2) which has shown high potency...
- Structure guided P1 ' modifications of HEA derived beta-secretase inhibitors for the treatment of Alzheimer's disease
[作者:Monenschein, H; Horne, DB; Bartberger, MD; Hitchcock, SA; Nguyen, TT; Patel, VF; Pennington, LD; Zhong, WG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3607-3611 , 文章类型: Article,,卷期:2012年22-11]
- The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off...
- New myrsinol diterpenes from Euphorbia prolifera and their inhibitory activities on LPS-induced NO production
[作者:Xu, J; Jin, DQ; Guo, YQ; Xie, CF; Ma, YG; Yamakuni, T; Ohizumi, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3612-3618 , 文章类型: Article,,卷期:2012年22-11]
- A phytochemical investigation of the roots of Euphorbia prolifera led to the isolation of ten new myrsinol diterpenes, named euphorbialoids A-J (1-10), and two known analogues (11 and 12). Their structures were elucidate...
- Artificial ladder-shaped polyethers that inhibit maitotoxin-induced Ca2+ influx in rat glioma C6 cells
[作者:Oishi, T; Konoki, K; Tamate, R; Torikai, K; Hasegawa, F; Matsumori, N; Murata, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3619-3622 , 文章类型: Article,,卷期:2012年22-11]
- Maitotoxin (MTX) is a ladder-shaped polyether produced by the epiphytic dinoflagellate Gambierdiscus toxicus. It is known to elicit potent toxicity against mammals and induce influx of Ca2+ into cells. An artificial ladd...
- Synthesis and antimicrobial activities of structurally novel S,S '-bis(heterosubstituted) disulfides
[作者:Ramaraju, P; Gergeres, D; Turos, E; Dickey, S; Lim, DV; Thomas, J; Anderson, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3623-3631 , 文章类型: Article,,卷期:2012年22-11]
- The central focus of this study is on the antibacterial and antifungal properties of synthetically produced S,S'-bis(heterosubstituted) disulfides as a means to control the growth of various infection-causing pathogens. ...
- A specific molecular beacon probe for the detection of human prostate cancer cells
[作者:Jiang, YL; McGoldrick, CA; Yin, DL; Zhao, J; Patel, V; Brannon, MF; Lightner, JW; Krishnan, K; Stone, WL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3632-3638 , 文章类型: Article,,卷期:2012年22-11]
- The small-molecule, water-soluble molecular beacon probe 1 is hydrolyzed by the lysate and living cells of human prostate cancer cell lines (LNCaP), resulting in strong green fluorescence. In contrast, probe 1 does not u...
- Discovery and evaluation of selective N-type calcium channel blockers: 6-Unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives
[作者:Yamamoto, T; Niwa, S; Tokumasu, M; Onishi, T; Ohno, S; Hagihara, M; Koganei, H; Fujita, S; Takeda, T; Saitou, Y; Iwayama, S; Takahara, A; Iwata, S; Shoji, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3639-3642 , 文章类型: Article,,卷期:2012年22-11]
- A structure-activity relationship study of 6-unsubstituted-1,4-dihydropyridine and 2,6-unsubstituted-1,4-dihydropyridine derivatives was conducted in an attempt to discover N-type calcium channel blockers that were highl...
- Design, synthesis, and structure-activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors
[作者:Kamata, M; Yamashita, T; Kina, A; Funata, M; Mizukami, A; Sasaki, M; Tani, A; Funami, M; Amano, N; Fukatsu, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3643-3647 , 文章类型: Article,,卷期:2012年22-11]
- Spiro-lactone (S)-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor and was found to be metabolically liable in human hepatic microsomes. To remove one of the risk factors in human study by improving the metabolic sta...
- Chlorin-PEI-labeled cellulose nanocrystals: Synthesis, characterization and potential application in PDT
[作者:Drogat, N; Granet, R; Le Morvan, C; Begaud-Grimaud, G; Krausz, P; Sol, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3648-3652 , 文章类型: Article,,卷期:2012年22-11]
- This Letter reports the synthesis and characterization of a new series of water-stable and soluble photosensitizers (PS-CNCs) composed of cellulose nanocrystals (CNCs) bearing polyaminated chlorin p6. With a view to impr...
- Synthesis of norlignans and in vitro inhibitory activity of antigen-induced degranulation
[作者:Park, E; Yang, YJ; Kim, A; Kwak, JH; Jung, YH; Kang, SC; Kim, IS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3653-3655 , 文章类型: Article,,卷期:2012年22-11]
- The synthesis and biological evaluation of a series of novel norlignans are described. Norlignans were evaluated for their inhibitory activity on the release of beta-hexosaminidase, a marker of degranulation, from RBL-2H...
- Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N '-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism
[作者:Bhondwe, RS; Kang, DW; Kim, MS; Kim, HS; Park, SG; Son, K; Choi, S; Kuhs, KAL; Pavlyukovets, VA; Pearce, LV; Blumberg, PM; Lee, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3656-3660 , 文章类型: Article,,卷期:2012年22-11]
- The structure-activity relationships of N-(3-acyloxy-2-benzylpropyl)-N'-4-[(methylsulfonylamino) benzyl] thioureas, which represent simplified RTX-based vanilloids, were investigated by varying the distances between the ...
- Synthetic menthyl alpha/beta-(1 -> 6)-diglucopyranosides-induced cell death in human leukemia cells is dependent on caspases
[作者:Marrero, MT; Tejera, S; Estevez, S; Quintana, J; Mayato, C; Dorta, RL; Vazquez, JT; Estevez, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3665-3670 , 文章类型: Article,,卷期:2012年22-11]
- A series of alkyl alpha/beta-(1 -> 6)-diglucopyranosides 1-12 were synthesized and assessed for cytotoxicity against HL-60, U937, Molt-3 and MCF-7 cancer cell lines. The menthyl derivatives displayed strong cytotoxic pro...
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