- Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease
[作者:Abdellatif, KRA; Velazquez, CA; Huang, ZJ; Chowdhury, MA; Knaus, EE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5245-5250 , 文章类型: Article,,卷期:2010年20-17]
- A group of (Z)-1,1-diphenyl-2-(4-methylsulfonylphenyl) alk-1-enes were synthesized using methodologies that will allow incorporation of a [C-11] OCH3 substituent at the para-position of the C-1 phenyl ring, a [C-11] SO2C...
- Synthesis and antituberculosis activity of new fatty acid amides
[作者:D'Oca, CDM; Coelho, T; Marinho, TG; Hack, CRL; Duarte, RD; da Silva, PA; D'Oca, MGM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5255-5257 , 文章类型: Article,,卷期:2010年20-17]
- This work reports the synthesis of new fatty acid amides from C16: 0, 18: 0, 18: 1, 18: 1 (OH), and 18: 2 fatty acids families with cyclic and acyclic amines and demonstrate for the first time the activity of these compo...
- Oxidative stimuli-responsive nanoprodrug of camptothecin kills glioblastoma cells
[作者:Lee, BS; Nalla, AK; Stock, IR; Shear, TC; Black, KL; Yu, JS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5262-5268 , 文章类型: Article,,卷期:2010年20-17]
- The purpose of this study was to prepare and characterize nanometer-sized prodrug (nanoprodrug) of camptothecin. The camptothecin prodrug was synthesized using tetraethylene glycol spacer linked via carbonate bond to cam...
- Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists
[作者:Zhong, M; Shen, W; Barr, KJ; Arbitrario, JP; Arkin, MR; Bui, M; Chen, T; Cunningham, BC; Evanchik, MJ; Hanan, EJ; Hoch, U; Huen, K; Hyde, J; Kumer, JL; Lac, T; Lawrence, CE; Martell, JR; Oslob, JD; Paulvannan, K; Prabhu, S; Silverman, JA; Wright, J; Yu, CH; Zhu, JA; Flanagan, WM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5269-5273 , 文章类型: Article,,卷期:2010年20-17]
- This letter describes the discovery of a novel series of tetrahydroisoquinoline (THIQ)-derived small molecules that potently inhibit both human T-cell migration and super-antigen induced T-cell activation through disrupt...
- Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists
[作者:Lange, JHM; Attali, A; van der Neut, MAW; Wals, HC; Mulder, A; Zilaout, H; Duursma, A; van Aken, HHM; van Vliet, BJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4992-4998 , 文章类型: Article,,卷期:2010年20-17]
- The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1-23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24-27 as two novel cannabinoid CB1 receptor agonist classes were described. The target...
- Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents
[作者:Yang, SH; Van, HTM; Le, TN; Khadka, DB; Cho, SH; Lee, KT; Chung, HJ; Lee, SK; Ahn, CH; Lee, YB; Cho, WJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5277-5281 , 文章类型: Article,,卷期:2010年20-17]
- In the search for potent water-soluble 3-arylisoquinolines, several 3-arylisoquinolinamines were designed and synthesized. Various substituted 3-arylisoquinolinamines exhibited strong cytotoxic activity against eight dif...
- Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library
[作者:Kurosumi, M; Nishio, Y; Osawa, S; Kobayashi, H; Iwatsubo, T; Tomita, T; Miyachi, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5282-5285 , 文章类型: Article,,卷期:2010年20-17]
- Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived gamma-secretase inhibitors (GSIs). Structure-activity relationship studies indicated tha...
- Biaryl substituted hydantoin compounds as TACE inhibitors
[作者:Yu, WS; Tong, L; Kim, SH; Wong, MKC; Chen, L; Yang, DY; Shankar, BB; Lavey, BJ; Zhou, GW; Kosinski, A; Rizvi, R; Li, DS; Feltz, RJ; Piwinski, JJ; Rosner, KE; Shih, NY; Siddiqui, MA; Guo, ZY; Orth, P; Shah, H; Sun, J; Umland, S; Lundell, DJ; Niu, XD; Kozlowski, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5286-5289 , 文章类型: Article,,卷期:2010年20-17]
- We disclose further optimization of hydantoin TNF-alpha convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds w...
- The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H-3 antagonists
[作者:Ting, PC; Lee, JF; Albanese, MM; Wu, J; Aslanian, R; Favreau, L; Nardo, C; Korfmacher, WA; West, RE; Williams, SM; Anthes, JC; Rivelli, MA; Corboz, MR; Hey, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5004-5008 , 文章类型: Article,,卷期:2010年20-17]
- A structure-activity relationship study of the lead piperazinylcarbonylpiperidine compound 3 resulted in the identification of 4-benzimidazolyl-piperidinylcarbonyl-piperidine 6h as a histamine-3 (H-3) receptor antagonist...
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