- Synthesis of novel long wavelength cationic chlorins via stereoselective aldol-like condensation
[作者:Li, JZ; Wang, JJ; Yoon, I; Cui, BC; Shim, YK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1846-1849 , 文章类型: Article,,卷期:2012年22-5]
- Using stereoselective aldol-like condensation as a key methodology, a series of chlorophyll a-based long wavelength cationic chlorins were synthesized using methyl pyropheophorbide a (MPPa) and purpurin-18-N-methoxylimid...
- Synthesis and biological evaluation of sulfonyl acrylonitriles as novel inhibitors to peritoneal carcinomatosis
[作者:Zificsak, CA; Shen, Y; Lisko, JG; Theroff, JP; Lao, XG; Bollt, O; Li, XF; Dorsey, BD; Kuwada, SK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1850-1853 , 文章类型: Article,,卷期:2012年22-5]
- The vast majority of cancer patients die from metastasis, the process by which cancer cells spread to secondary tissues through body fluids. Peritoneal carcinomatosis is a type of metastasis in which cancer cells gain ac...
- Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy
[作者:Swahn, BM; Holenz, J; Kihlstrom, J; Kolmodin, K; Lindstrom, J; Plobeck, N; Rotticci, D; Sehgelmeble, F; Sundstrom, M; von Berg, S; Falting, J; Georgievska, B; Gustavsson, S; Neelissen, J; Ek, M; Olsson, LL; Berg, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1854-1859 , 文章类型: Article,,卷期:2012年22-5]
- The evaluation of a series of bicyclic aminoimidazoles as potent BACE-1 inhibitors is described. The crystal structures of compounds 14 and 23 in complex with BACE-1 reveal hydrogen bond interactions with the protein imp...
- Characterization of TAE684 as a potent LRRK2 kinase inhibitor
[作者:Zhang, JW; Deng, XM; Choi, HG; Alessi, DR; Gray, NS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1864-1869 , 文章类型: Article,,卷期:2012年22-5]
- Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of ana...
- Identification of fused bicyclic heterocycles as potent and selective 5-HT2A receptor antagonists for the treatment of insomnia
[作者:Xiong, YF; Ullman, B; Choi, JSK; Cherrier, M; Strah-Pleynet, S; Decaire, M; Feichtinger, K; Frazer, JM; Yoon, WH; Whelan, K; Sanabria, EK; Grottick, AJ; Al-Shamma, H; Semple, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1870-1873 , 文章类型: Article,,卷期:2012年22-5]
- A series of fused bicyclic heterocycles was identified as potent and selective 5-HT2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, go...
- Imidazo[1,2-a] pyrazines as novel PI3K inhibitors
[作者:Gonzalez, SM; Hernandez, AI; Varela, C; Rodriguez-Aristegui, S; Alvarez, RM; Garcia, AB; Lorenzo, M; Rivero, V; Oyarzabal, J; Rabal, O; Bischoff, JR; Albarran, M; Cebria, A; Alfonso, P; Link, W; Fominaya, J; Pastor, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1874-1878 , 文章类型: Article,,卷期:2012年22-5]
- Phosphoinositide-3-kinase (PI3K) is an important target for cancer therapeutics due to the deregulation of its signaling pathway in a wide variety of human cancers. We describe herein a novel series of imidazo[1,2-a]pyra...
- Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
[作者:Kelly, JM; Taylor, MC; Horn, D; Loza, E; Kalvinsh, I; Bjorkling, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1886-1890 , 文章类型: Article,,卷期:2012年22-5]
- A number of hydroxamic acid derivatives which inhibit human histone deacetylases were investigated for efficacy against cultured bloodstream form Trypanosoma brucei. Three out of the four classes tested displayed signifi...
- Structure-activity relationship of the 7-hydroxy benzimidazole analogs as glycogen synthase kinase 3 beta inhibitor
[作者:Lee, SC; Shin, D; Cho, JM; Ro, S; Suh, YG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1891-1894 , 文章类型: Article,,卷期:2012年22-5]
- Design, synthesis and the GSK3 beta inhibitory activities of the 7-hydroxy benzimidazole analogs are described. The solid-phase synthetic route was also developed for preparation of the analogs consisting of the novel AT...
- New antitumor compounds from Carya cathayensis
[作者:Wu, W; Bi, XL; Cao, JQ; Zhang, KQ; Zhao, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1895-1898 , 文章类型: Article,,卷期:2012年22-5]
- A new lignan (7R,8S,8 ' R)-4,4 ',9-trihydroxy-7,9 '-epoxy-8,8 '-lignan, and three new phenolics, carayensin-A, carayensin-B, and carayensin-C, together with 13 known compounds were isolated from the shells of Carya catha...
- Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at the delta opioid receptor. Discovery of two highly potent and selective delta opioid agonists
[作者:Berezowska, I; Lemieux, C; Chung, NN; Ding, JG; Schiller, PW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1899-1902 , 文章类型: Article,,卷期:2012年22-5]
- Analogues of the delta opioid antagonist peptide TIPP (H-Tyr-Tic-Phe-Phe-OH; Tic = 1,2,3,4-tetrahydroisoquinoline3-carboxylic acid) containing various 4 '-[N-(alkyl or aralkyl) carboxamido] phenylalanine analogues in pla...
- Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia
[作者:Calvo, RR; Meegalla, SK; Parks, DJ; Parsons, WH; Ballentine, SK; Lubin, ML; Schneider, C; Colburn, RW; Flores, CM; Player, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1903-1907 , 文章类型: Article,,卷期:2012年22-5]
- Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonist...
- New cyclic peptides with osteoblastic proliferative activity from Dianthus superbus
[作者:Tong, Y; Luo, JG; Wang, R; Wang, XB; Kong, LY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1908-1911 , 文章类型: Article,,卷期:2012年22-5]
- Two new cyclic peptides, dianthins G-H (1 and 2), together with the known dianthin E (3), were isolated from the traditional Chinese medicinal plant Dianthus superbus. The sequences of cyclic peptides 1 and 2 were elucid...
- 1,2,4-Oxadiazoles: A new class of anti-prostate cancer agents
[作者:Khatik, GL; Kaur, J; Kumar, V; Tikoo, K; Nair, VA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1912-1916 , 文章类型: Article,,卷期:2012年22-5]
- Sulfide and sulfonyl derivatives of 1,2,4-oxadiazoles were synthesized and screened by MTT assay on the prostate cancer cells, DU-145. Six compounds were identified as potential anti-prostate cancer agents with IC50 valu...
- Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents
[作者:Alegaon, SG; Alagawadi, KR; Sonkusare, PV; Chaudhary, SM; Dadwe, DH; Shah, AS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1917-1921 , 文章类型: Article,,卷期:2012年22-5]
- The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacterium tuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial ...
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