- Synthesis, anticancer activity and apoptosis inducing ability of bisindole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates
[作者:Kamal, A; Srikanth, YVV; Ramaiah, MJ; Khan, MNA; Reddy, MK; Ashraf, M; Lavanya, A; Pushpavalli, SNCVL; Pal-Bhadra, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:571-578 , 文章类型: Article,,卷期:2012年22-1]
- A series of bisindole-pyrrolobenzodiazepine conjugates (5a-f) linked through different alkane spacers was prepared and evaluated for their anticancer activity. All compounds exhibited significant anticancer potency and t...
- The novel agent ophiobolin O induces apoptosis and cell cycle arrest of MCF-7 cells through activation of MAPK signaling pathways
[作者:Yang, TT; Lu, ZY; Meng, L; Wei, SJ; Hong, K; Zhu, WM; Huang, CG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:579-585 , 文章类型: Article,,卷期:2012年22-1]
- Ophiobolin O is a natural compound that has been isolated from Aspergillus ustus 094102. This is the first study to demonstrate the anti-proliferative effect of ophiobolin O in human breast cancer MCF-7 cells. The result...
- Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD)
[作者:Wu, YC; Li, JC; Wu, JJ; Morgan, P; Xu, X; Rancati, F; Vallese, S; Raveglia, L; Hotchandani, R; Fuller, N; Bard, J; Cunningham, K; Fish, S; Krykbaev, R; Tam, S; Goldman, SJ; Williams, C; Mansour, TS; Saiah, E; Sypek, J; Li, W,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:138-143 , 文章类型: Article,,卷期:2012年22-1]
- Chronic obstructive pulmonary disease (COPD) is an inflammatory lung disease associated with irreversible progressive airflow limitation. Matrix metalloproteinase-12 (MMP-12) has been characterized to be one of the major...
- Structure-activity relationship studies of S1P agonists with a dihydronaphthalene scaffold
[作者:Kurata, H; Kusumi, K; Otsuki, K; Suzuki, R; Kurono, M; Tokuda, N; Takada, Y; Shioya, H; Mizuno, H; Komiya, T; Ono, T; Hagiya, H; Minami, M; Nakade, S; Habashita, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:144-148 , 文章类型: Article,,卷期:2012年22-1]
- Structure-activity relationship (SAR) of sphingosine-1-phosphate receptor agonists with a dihydronaphthalene scaffold was investigated. Compound 1 was modified to improve S1P(1) agonistic activity and in vivo peripheral ...
- Synthesis and in vitro and in vivo anticancer activity of novel phenylmethylene bis-isoxazolo[4,5-b]azepines
[作者:Rajanarendar, E; Reddy, MN; Murthy, KR; Surendar, P; Reddy, RN; Reddy, YN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:149-153 , 文章类型: Article,,卷期:2012年22-1]
- A series of novel phenylmethylene bis-isoxazolo[4,5-b] azepine derivatives (10) have been synthesized from 3-methyl-4-nitro-5-styrylisoxazoles 6. The reaction of 6 with 3,5-dimethyl-4-nitroisoxazole (7) in piperidine aff...
- Discovery of estrogen receptor alpha modulators from natural compounds in Si-Wu-Tang series decoctions using estrogen-responsive MCF-7 breast cancer cells
[作者:Liu, L; Ma, HY; Tang, YP; Chen, WX; Lu, Y; Guo, JM; Duan, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:154-163 , 文章类型: Article,,卷期:2012年22-1]
- The binding between the estrogen receptor alpha (ER-alpha) and a variety of compounds in traditional Chinese formulae, Si-Wu-Tang (SWT) series decoctions, was studied using a stably-transfected human breast cancer cell l...
- Synthesis and biological evaluation of molecular probes based on the 9-methylstreptimidone derivative DTCM-glutarimide
[作者:Ota, E; Takeiri, M; Tachibana, M; Ishikawa, Y; Umezawa, K; Nishiyama, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:164-167 , 文章类型: Article,,卷期:2012年22-1]
- Molecular probes based on 3-[(dodecylthiocarbonyl)methyl]glutarimide (DTCM-glutarimide) were synthesized and assessed for inhibitory activity against LPS-induced NO production. Among the probes examined, several derivati...
- Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay
[作者:Wang, D; Wang, F; Tan, YX; Dong, LW; Chen, L; Zhu, WL; Wang, HY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:168-171 , 文章类型: Article,,卷期:2012年22-1]
- In this study, six novel dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) inhibitors with IC(50) values ranging from 1.51 to 88.13 mu M were successfully identified through virtual screening and in ...
- Maplexins, new alpha-glucosidase inhibitors from red maple (Acer rubrum) stems
[作者:Wan, CP; Yuan, T; Li, LY; Kandhi, V; Cech, NB; Xie, MY; Seeram, NP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:597-600 , 文章类型: Article,,卷期:2012年22-1]
- Thirteen gallic acid derivatives including five new gallotannins, named maplexins A-E, were isolated from red maple (Acer rubrum) stems. The compounds were identified by spectral analyses. The maplexins varied in number ...
- Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase
[作者:Pecic, S; Deng, SX; Morisseau, C; Hammock, BD; Landry, DW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:601-605 , 文章类型: Article,,卷期:2012年22-1]
- Inhibition of soluble epoxide hydrolase (sEH) has been proposed as a new pharmaceutical approach for treating hypertension and vascular inflammation. The most potent sEH inhibitors reported in literature to date are urea...
- Methylenebissantin: A rare methylene-bridged bisflavonoid from Dodonaea viscosa which inhibits Plasmodium falciparum enoyl-ACP reductase
[作者:Muhammad, A; Anis, I; Ali, Z; Awadelkarim, S; Khan, A; Khalid, A; Shah, MR; Galal, M; Khan, IA; Choudhary, MI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:610-612 , 文章类型: Article,,卷期:2012年22-1]
- A new methylene-bridged bisflavonoid, methylenebissantin (1), and nine known compounds, including flavonoids (2-5), diterpenoids (6 and 7), and phenol derivatives (8-10) were isolated from the aerial parts of Dodonaea vi...
- Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series
[作者:Oubrie, A; Kaptein, A; de Zwart, E; Hoogenboom, N; Goorden, R; van de Kar, B; van Hoek, M; de Kimpe, V; van der Heijden, R; Borsboom, J; Kazemier, B; de Roos, J; Scheffers, M; Lommerse, J; Schultz-Fademrecht, C; Barf, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:613-618 , 文章类型: Article,,卷期:2012年22-1]
- Optimization of our previously described pyrrolopiperidone series led to the identification of a new benzamide sub-series, which exhibits consistently high potency in biochemical and cell-based assays throughout the seri...
- Chromenones as potent bradykinin B1 antagonists
[作者:Bryan, MC; Biswas, K; Peterkin, TAN; Rzasa, RM; Arik, L; Lehto, SG; Sun, H; Hsieh, FY; Xu, C; Fremeau, RT; Allen, JR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:619-622 , 文章类型: Article,,卷期:2012年22-1]
- A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. ...
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