- Synthesis and anticancer evaluation of thiazolyl-chalcones
[作者:Shi, HB; Zhang, SJ; Ge, QF; Guo, DW; Cai, CM; Hu, WX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6555-6559 , 文章类型: Article,,卷期:2010年20-22]
- Thirty-seven (E)-1-(4-methyl-2-arylaminothiazol-5-yl)-3-arylprop-2-en-1-ones were synthesized via Claisen-Schmidt condensation of 1-(4-methyl-2-(arylamino)thiazol-5-yl) ethanone with the corresponding arylaldehydes. All ...
- Inhibition of Bfl-1 with N-aryl maleimides
[作者:Cashman, JR; MacDonald, M; Ghirmai, S; Okolotowicz, KJ; Sergienko, E; Brown, B; Garcia, X; Zhai, DY; Dahl, R; Reed, JC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6560-6564 , 文章类型: Article,,卷期:2010年20-22]
- High-throughput screening of 66,000 compounds using competitive binding of peptides comprising the BH3 domain to anti-apoptotic Bfl-1 led to the identification of 14 validated 'hits' as inhibitors of Bfl-1. N-Aryl maleim...
- Polymerase-directed synthesis of C5-ethynyl locked nucleic acids
[作者:Veedu, RN; Burri, HV; Kumar, P; Sharma, PK; Hrdlicka, PJ; Vester, B; Wengel, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6565-6568 , 文章类型: Article,,卷期:2010年20-22]
- Modified nucleic acids have considerable potential in nanobiotechnology for the development of nanomedicines and new materials. Locked nucleic acid (LNA) is one of the most prominent nucleic acid analogues reported so fa...
- Kojyl thioether derivatives having both tyrosinase inhibitory and anti-inflammatory properties
[作者:Rho, HS; Ahn, SM; Yoo, DS; Kim, MK; Cho, DH; Cho, JY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6569-6571 , 文章类型: Article,,卷期:2010年20-22]
- This study was conducted to examine the tyrosinase inhibitory and anti-inflammatory activities of kojic acid derivatives. A series of kojic acid derivatives containing thioether, sulfoxide, and sulfone linkages were synt...
- Triazolyl tryptoline derivatives as beta-secretase inhibitors
[作者:Jiaranaikulwanitch, J; Boonyarat, C; Fokin, VV; Vajragupta, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6572-6576 , 文章类型: Article,,卷期:2010年20-22]
- Tryptoline, a core structure of ochrolifuanine E, which is a hit compound from virtual screening of the Thai herbal database against BACE1 was used as a scaffold for the design of BACE1 inhibitors. The tryptoline was lin...
- Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality
[作者:Wood, MR; Schirripa, KM; Kim, JJ; Bednar, RA; Fay, JF; Bruno, JG; Moore, EL; Mosser, SD; Roller, S; Salvatore, CA; Vacca, JP; Selnick, HG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6827-6830 , 文章类型: Article,,卷期:2010年20-22]
- A previously utilized quinoline-for-N-phenylamide replacement strategy was employed against a central amide in a novel class of CGRP receptor antagonists. A unique and unexpected substitution pattern was ultimately requi...
- Design, synthesis and reactivity of C-2-symmetric azobenzene-based amino acid-bis(propargyl sulfones)
[作者:Mitra, D; Banerjee, DR; Das, AK; Basak, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6831-6835 , 文章类型: Article,,卷期:2010年20-22]
- C-2-Symmetric azobenzene-amino acid linked bis(propargyl sulfones) 1 and 2 containing stable E azo moiety have been synthesized. Upon irradiation with long wavelength UV these compounds isomerized to the Z-form, whose th...
- Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ETA antagonists
[作者:Patel, HJ; Olgun, N; Lengyel, I; Reznik, S; Stephani, RA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6840-6844 , 文章类型: Article,,卷期:2010年20-22]
- A series of 1,3,6-trisubsituted-4-oxo-1,4-dihyroquinoline-2-carboxylic acid analogs (2a-m) were designed and synthesized and their pharmacological activity determined, with the objective to better understand their SAR as...
- Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists
[作者:McGuinness, BF; Cole, AG; Dong, G; Brescia, MR; Shao, Y; Henderson, I; Rokosz, LL; Stauffer, TM; Mannava, N; Kimble, EF; Hicks, C; White, N; Wines, PG; Quadros, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6845-6849 , 文章类型: Article,,卷期:2010年20-22]
- A novel series of adenosine A(2A) receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A(2A) binding affinity, A(1) selecti...
- Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy
[作者:Jiao, GS; Kim, S; Moayeri, M; Cregar-Hernandez, L; McKasson, L; Margosiak, SA; Leppla, SH; Johnson, AT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6850-6853 , 文章类型: Article,,卷期:2010年20-22]
- Sub-nanomolar small molecule inhibitors of anthrax lethal factor have been identified using SAR and Merck L915 (4) as a model compound. One of these compounds (16) provided 100% protection in a rat lethal toxin model of ...
- Development of the next generation of HIV-1 integrase inhibitors: Pyrazolone as a novel inhibitor scaffold
[作者:Hadi, V; Koh, YH; Sanchez, TW; Barrios, D; Neamati, N; Jung, KW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6854-6857 , 文章类型: Article,,卷期:2010年20-22]
- HIV-1 integrase (IN), one of the essential enzymes in HIV infection, has been validated as a target for HIV treatment. While more than 20 drugs have been approved by the FDA to treat HIV/AIDS, only one drug, Raltegravir ...
- Deconstructing estradiol: Removal of B-ring generates compounds which are potent and subtype-selective estrogen receptor agonists (vol 19, pg 1250, 2009)
[作者:Asim, M; El-Salfiti, M; Qian, YM; Choueiri, C; Salari, S; Cheng, J; Shadnia, H; Bal, M; Pratt, MAC; Carlson, KE; Katzenellenbogen, JA; Wright, JS; Durst, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6861-6862 , 文章类型: Correction,,卷期:2010年20-22]
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- Total synthesis of (+/-)-elegansidiol, (+/-)-farnesiferol B and (+/-)-farnesiferol D (vol 20, pg 3814, 2010)
[作者:Yadav, JS; Satyanarayana, K; Sreedhar, P; Srihari, P; Shaik, TB; Kalivendi, SV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6863-6863 , 文章类型: Correction,,卷期:2010年20-22]
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