- New C-23 modified of silybin and 2,3-dehydrosilybin: Synthesis and preliminary evaluation of antioxidant properties
[作者:Zarrelli, A; Sgambato, A; Petito, V; De Napoli, L; Previtera, L; Di Fabio, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4389-4392 , 文章类型: Article,,卷期:2011年21-15]
- Silybin is the major flavonolignan of silymarin and it displays a plethora of biological effects, generally ascribed to its antioxidant properties. Herein we shall describe an efficient synthetic strategy to obtain a var...
- Construction of a (19)F-lectin biosensor for glycoprotein imaging by using affinity-guided DMAP chemistry
[作者:Sun, Y; Takaoka, Y; Tsukiji, S; Narazaki, M; Matsuda, T; Hamachi, I,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4393-4396 , 文章类型: Article,,卷期:2011年21-15]
- In this study, assisted by affinity-guided DMAP strategy, we developed a novel (19)F-modified lectin as a biosensor for specific detection and imaging of glycoproteins. Exploited the large chemical shift anisotropy prope...
- Nothospondin, a new AP-1 inhibitory quassinoid from the Cameroonian plant Nothospondias staudtii
[作者:Diyabalanage, T; Ratnayake, R; Wilson, JA; Henrich, CJ; Beutler, JA; Colburn, NH; McMahon, JB; Gustafson, KR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4397-4399 , 文章类型: Article,,卷期:2011年21-15]
- A high throughput screen for inhibitors of the oncogenic transcription factor activator protein-1 (AP-1) was applied to the NCI repository of natural product extracts. The liphophilic extract of the plant Nothospondias s...
- Flavans from Iris tenuifolia and their effects on beta-amyloid aggregation and neural stem cells proliferation in vitro
[作者:Cui, YM; Wang, H; Liu, QR; Han, M; Lu, Y; Zhao, CQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4400-4403 , 文章类型: Article,,卷期:2011年21-15]
- Two new flavans (1, 2) and a new flavanone (3), together with three known compounds (4-6), were isolated from the roots of Iris tenuifolia. Their structures were elucidated by means of spectroscopic methods including 1D ...
- Synthesis, molecular modeling and bio-evaluation of cycloalkyl fused 2-aminopyrimidines as antitubercular and antidiabetic agents
[作者:Singh, N; Pandey, SK; Anand, N; Dwivedi, R; Singh, S; Sinha, SK; Chaturvedi, V; Jaiswal, N; Srivastava, AK; Shah, P; Siddiqui, MI; Tripathi, RP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4404-4408 , 文章类型: Article,,卷期:2011年21-15]
- An economical and efficient one step synthesis of a series of 8-(arylidene)-4-(aryl)-5,6,7,8-tetrahydroquinazolin-2-ylamines and 9-(arylidene)-4-(aryl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-2-ylamines by the reaction...
- Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent
[作者:Kerns, JK; Nie, H; Bondinell, W; Widdowson, KL; Yamashita, DS; Rahman, A; Podolin, PL; Carpenter, DC; Jin, Q; Riflade, B; Dong, XY; Nevins, N; Keller, PM; Mitchell, L; Tomaszek, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4409-4415 , 文章类型: Article,,卷期:2011年21-15]
- A series of azepanone inhibitors of cathepsin S is described. Selectivity over both cathepsin K and cathepsin L was achieved by varying the P2 substituent. Ultimately, a balanced potency and selectivity profile was achie...
- Antiproliferative activity and QSAR studies of a series of new 4-aminomethylidene derivatives of some pyrazol-5-ones
[作者:Markovic, V; Eric, S; Stanojkovic, T; Gligorijevic, N; Arandelovic, S; Todorovic, N; Trifunovic, S; Manojlovic, N; Jelic, R; Joksovic, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4416-4421 , 文章类型: Article,,卷期:2011年21-15]
- Twenty five 4-aminomethylidene derivatives obtained from 3-phenyl-2-pyrazolin-5-one and 1,3-diphenyl-2-pyrazolin-5-one were synthesized and tested for their antiproliferative activity against human breast cancer MDA-MB-3...
- Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 1
[作者:Malancona, S; Altamura, S; Filocamo, G; Kinzel, O; Ignacio, J; Hernando, M; Rowley, M; Scarpelli, R; Steinkuhler, C; Jones, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4422-4428 , 文章类型: Article,,卷期:2011年21-15]
- The Hedgehog (Hh-) signaling pathway is a key developmental pathway which controls patterning, growth and cell migration in most tissues, but evidence has accumulated showing that many human tumors aberrantly reactivate ...
- Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a] pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2
[作者:Kinzel, O; Alfieri, A; Altamura, S; Brunetti, M; Bufali, S; Colaceci, F; Ferrigno, F; Filocamo, G; Fonsi, M; Gallinari, P; Malancona, S; Hernando, JIM; Monteagudo, E; Orsale, MV; Palumbi, MC; Pucci, V; Rowley, M; Sasso, R; Scarpelli, R; Steinkuhler, C; Jones, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4429-4435 , 文章类型: Article,,卷期:2011年21-15]
- The Hedgehog (Hh-) signaling pathway is a key developmental pathway which gets reactivated in many human tumors, and smoothened (Smo) antagonists are emerging as novel agents for the treatment of malignancies dependent o...
- Development of potent B-Raf(V600E) inhibitors containing an arylsulfonamide headgroup
[作者:Stellwagen, JC; Adjabeng, GM; Arnone, MR; Dickerson, SH; Han, C; Hornberger, KR; King, AJ; Mook, RA; Petrov, KG; Rheault, TR; Rominger, CM; Rossanese, OW; Smitheman, KN; Waterson, AG; Uehling, DE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4436-4440 , 文章类型: Article,,卷期:2011年21-15]
- A potent series of inhibitors against the B-RafV600E kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an aryl...
- New isoprenylated flavonoids and adipogenesis-promoting constituents from Morus notabilis
[作者:Hu, X; Ji, J; Wang, M; Wu, JW; Zhao, QS; Wang, HY; Hou, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4441-4446 , 文章类型: Article,,卷期:2011年21-15]
- Five new isoprenylated flavonoids, notabilisins A-E (1-5), and two known Diels-Alder adducts (6 and 7), were isolated from the twigs of Morus notabilis. Compounds 4 and 5 possess two novel pyran rings, which may be bioge...
- N-beta-Glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII
[作者:Rodriguez, OM; Maresca, A; Tempera, CA; Bravo, RD; Colinas, PA; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4447-4450 , 文章类型: Article,,卷期:2011年21-15]
- The transmembrane isoforms of carbonic anhydrase (CA IX and XII) have been shown to be linked to carcinogenesis and their inhibition to arrest primary tumor and metastases growth. In this Letter, we present a series of p...
- Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues
[作者:Ahsan, MJ; Samy, JG; Dutt, KR; Agrawal, UK; Yadav, BS; Vyas, S; Kaur, R; Yadav, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4451-4453 , 文章类型: Article,,卷期:2011年21-15]
- In the present investigation, a series of 3-substituted-N-aryl-6,7-dimethoxy-3a, 4-dihydro-3-Hindeno[1,2-c]pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold seri...
- Synthesis and antihistamine evaluations of novel loratadine analogues
[作者:Wang, Y; Wang, J; Lin, Y; Si-Ma, LF; Wang, DH; Chen, LG; Liu, DK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4454-4456 , 文章类型: Article,,卷期:2011年21-15]
- A series of loratadine analogues containing hydroxyl group and chiral center were synthesized. The effect of the synthesized compounds on the histamine-induced contractions of guinea-pig ileum muscles was studied. In add...
- Structure-activity study on a series of alpha-glutamic acid scaffold based compounds as new ADAMTS inhibitors
[作者:Peng, LJ; Duan, L; Liu, XF; Shen, MJ; Li, YJ; Yan, JJ; Li, HL; Ding, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4457-4461 , 文章类型: Article,,卷期:2011年21-15]
- A series of alpha-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4-oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activiti...
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