- Synthesis and evaluation of anti-thrombotic activity of benzocoumarin amide derivatives
[作者:Sashidhara, KV; Palnati, GR; Avula, SR; Singh, S; Jain, M; Dikshit, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3115-3121 , 文章类型: Article,,卷期:2012年22-9]
- A series of novel benzocoumarin amide derivatives have been synthesized and evaluated for their antithrombotic activity. Amongst these, compounds 5, 7 and 8 exhibited promising anti-thrombotic profile in an established m...
- Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents
[作者:Liu, T; Sun, CY; Xing, XM; Jing, LL; Tan, R; Luo, YF; Huang, WC; Song, H; Li, ZC; Zhao, YL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3122-3125 , 文章类型: Article,,卷期:2012年22-9]
- A novel class of acetylhydrazone derivatives (5a-x) containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moieties are synthesizer, and their antitumor activities against A549, HCT116, HepG2, PC-9, and A375 were determi...
- Cytotoxic cytochalasins from the endozoic fungus Phoma sp of the giant jellyfish Nemopilema nomurai
[作者:La Kim, E; Li, JL; Dang, HT; Hong, J; Lee, CO; Kim, DK; Yoon, WD; Kim, E; Liu, YH; Jung, JH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3126-3129 , 文章类型: Article,,卷期:2012年22-9]
- Four new cytochalasin derivatives (1-4), together with cytochalasin B (5), were isolated from the fungus Phoma sp. obtained from the giant jellyfish Nemopilema nomurai. The planar structure and relative stereo-chemistry ...
- Nelumal A, the active principle from Ligularia nelumbifolia, is a novel farnesoid X receptor agonist
[作者:Epifano, F; Genovese, S; Squires, EJ; Gray, MA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3130-3135 , 文章类型: Article,,卷期:2012年22-9]
- A series of 29 oxyprenylated and azoprenylated phenylpropanoids were chemically synthesized and tested in transfected cultured HepG2 cells by means of the dual-luciferase assay as farnesoid X receptor (FXR) agonists, usi...
- Triazoloamides as potent gamma-secretase modulators with reduced hERG liability
[作者:Fischer, C; Zultanski, SL; Zhou, H; Methot, JL; Shah, S; Nuthall, H; Hughes, BL; Smotrov, N; Hill, A; Szewczak, AA; Moxham, CM; Bays, N; Middleton, RE; Munoz, B; Shearman, MS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3140-3146 , 文章类型: Article,,卷期:2012年22-9]
- Synthesis and SAR studies of novel aryl triazoles as gamma secretase modulators (GSMs) are presented in this communication. Starting from our aryl triazole leads, optimization studies were continued and the series progre...
- The facile synthesis of multifunctional PAMAM dendrimer conjugates through copper-free click chemistry
[作者:Huang, BH; Kukowska-Latallo, JF; Tang, SZ; Zong, H; Johnson, KB; Desai, A; Gordon, CL; Leroueil, PR; Baker, JR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3152-3156 , 文章类型: Article,,卷期:2012年22-9]
- The facile conjugation of three azido modified functionalities, namely a therapeutic drug (methotrexate), a targeting moiety (folic acid), and an imaging agent (fluorescein) with a G5 PAMAM dendrimer scaffold with cycloo...
- Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists
[作者:Sasmal, S; Balaji, G; Reddy, HRK; Balasubrahmanyam, D; Srinivas, G; Kyasa, S; Sasmal, PK; Khanna, I; Talwar, R; Suresh, J; Jadhav, VP; Muzeeb, S; Shashikumar, D; Reddy, KH; Sebastian, VJ; Frimurer, TM; Rist, O; Elster, L; Hogberg, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3157-3162 , 文章类型: Article,,卷期:2012年22-9]
- Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic and CNS disorders. The modeling-supported design, synthesis and multi-parameter optimization (biological ac...
- Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2
[作者:Sasmal, S; Balasubrahmanyam, D; Reddy, HRK; Balaji, G; Srinivas, G; Cheera, S; Abbineni, C; Sasmal, PK; Khanna, I; Sebastian, VJ; Jadhav, VP; Singh, MP; Talwar, R; Suresh, J; Shashikumar, D; Reddy, KH; Sihorkar, V; Frimurer, TM; Rist, O; Elster, L; Hogberg, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3163-3167 , 文章类型: Article,,卷期:2012年22-9]
- Melanin concentrating hormone receptor 1 (MCHR1) antagonists have potential for the treatment of obesity and several CNS disorders. In the preceding article, we have described a novel series of quinazolines as MCHR1 anta...
- Synthesis and characterization of pyruvate-isoniazid analogs and their copper complexes as potential ICL inhibitors
[作者:Shingnapurkar, D; Dandawate, P; Anson, CE; Powell, AK; Afrasiabi, Z; Sinn, E; Pandit, S; Swamy, KV; Franzblau, S; Padhye, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3172-3176 , 文章类型: Article,,卷期:2012年22-9]
- Currently used anti-tubercular drugs target actively growing Mycobacterium tuberculosis (Mtb) but there are no current therapies targeting persistent mycobacteria. Isocitrate lyase (ICL) is an important enzyme of the gly...
- The effects of diketopiperazines from Callyspongia sp on release of cytokines and chemokines in cultured J774A.1 macrophages
[作者:Chen, JH; Lan, XP; Liu, YH; Jia, AQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3177-3180 , 文章类型: Article,,卷期:2012年22-9]
- Diketopiperazines (DKPs) are a class of secondary metabolites that result from peptide bonds between two amino acids to form a lactam. Due to their rigid structure, chiral nature, and varied side chains, DKPs have been o...
- Discovery of a novel acetylcholinesterase inhibitor by structure-based virtual screening techniques
[作者:Chen, Y; Fang, L; Peng, SX; Liao, H; Lehmann, J; Zhang, YH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3181-3187 , 文章类型: Article,,卷期:2012年22-9]
- Acetylcholinesterase (AChE) is considered to be one of the most important targets for the treatment of Alzheimer's disease (AD). Previously our group has reported a series of tacrine-based hybrids as potent AChE inhibito...
- Pyronepolyene C-glucosides with NF-kappa B inhibitory and anti-influenza A viral (H1N1) activities from the sponge-associated fungus Epicoccum sp JJY40
[作者:Peng, JX; Jiao, JY; Li, J; Wang, W; Gu, QQ; Zhu, TJ; Li, DH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3188-3190 , 文章类型: Article,,卷期:2012年22-9]
- A new pyronepolyene C-glucoside, named iso-D8646-2-6 (1) together with the known related compound D8646-2-6 (2), was isolated from the sponge-associated fungus Epicoccum sp. JJY40. They showed NF-kappa B inhibitory and a...
- Synthesis and antitumor-evaluation of 1,3,4-thiadiazole-containing benzisoselenazolone derivatives
[作者:Luo, ZH; Chen, BQ; He, SY; Shi, YP; Liu, YM; Li, CW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3191-3193 , 文章类型: Article,,卷期:2012年22-9]
- A series of novel 1,3,4-thiadiazole-containing benzisoselenazolone derivatives were prepared by the condensation of 2-chloroselenobenzoyl chloride and 2-amino-5-substituted-1,3,4-thiadiazole. Their in vitro antiprolifera...
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