- Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transporter 1 (DMT1)
[作者：Cadieux, JA; Zhang, ZH; Mattice, M; Brownlie-Cutts, A; Fu, JM; Ratkay, LG; Kwan, R; Thompson, J; Sanghara, J; Zhong, J; Goldberg, YP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：90-95 , 文章类型： Article，,卷期：2012年22-1]
- Three distinct series of substituted pyrazole blockers of divalent metal transporter 1 (DMT1) were elaborated from the high-throughput screening pyrazolone hit 1. Preliminary hit-to-lead efforts revealed a preference for...
- 5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro- pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors
[作者：Caruso, M; Valsasina, B; Ballinari, D; Bertrand, J; Brasca, MG; Caldarelli, M; Cappella, P; Fiorentini, F; Gianellini, LM; Scolaro, A; Beria, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：96-101 , 文章类型： Article，,卷期：2012年22-1]
- The discovery and characterization of two new chemical classes of potent and selective Polo-like kinase 1 (PLK1) inhibitors is reported. For the most interesting compounds, we discuss the biological activities, crystal s...
- Imidazo [4,5f][1,10] phenanthroline derivatives as inhibitor of c-myc gene expression in A549 cells via NF-kappa B pathway
[作者：Sun, DD; Wang, WZ; Mao, JW; Mei, WJ; Liu, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：102-105 , 文章类型： Article，,卷期：2012年22-1]
- 1,10-Phenanthroline has been shown to exhibit anticancer activity. Here, a series of imidazo [4,5f][1,10] phenanthroline derivatives 1-10 were synthesized and their biological activities were further elucidated. We found...
- Fatty acyl-gramicidin S derivatives with both high antibiotic activity and low hemolytic activity
[作者：Tamaki, M; Fujinuma, K; Harada, T; Takanashi, K; Shindo, M; Kimura, M; Uchida, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：106-109 , 文章类型： Article，,卷期：2012年22-1]
- In the present study, novel eight GS derivatives having the octanoyl-(Lys)(n)-moieties, cyclo{-Val-Orn-Leu-D-Phe-Pro(4 beta-NH-X)-Val-Orn-Leu-D-Phe-Pro-} {X = -H (1), and -(Lys)(n)-CO(CH(2))(6)CH(3) n = 0 (2), 1 (3), 2 (...
- Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase
[作者：Yu, B; Tang, LD; Li, YL; Song, SH; Ji, XL; Lin, MS; Wu, CF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：110-114 , 文章类型： Article，,卷期：2012年22-1]
- We report herein the design and synthesis of novel 4-aminoquinazoline derivatives based on the inhibitors of VEGFR-2 tyrosine kinases. The VEGFR-2 inhibitory activities of these newly synthesized compounds were also eval...
- OFF-to-ON type fluorescent probe for the detection of 8-oxo-dG in DNA by the Adap-masked ODN probe
[作者：Taniguchi, Y; Koga, Y; Fukabori, K; Kawaguchi, R; Sasaki, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：543-546 , 文章类型： Article，,卷期：2012年22-1]
- We have recently reported that Adap (adenosine-1,3-diazaphenoxazine) is an artificial nucleoside analogue for the specific recognition by multiple hydrogen bonding and that its fluorescence is selectively quenched with 8...
- 5-Sulfonyl-benzimidazoles as selective CB2 agonists-Part 2
[作者：Gijsen, HJM; De Cleyn, MAJ; Surkyn, M; Van Lommen, GRE; Verbist, BMP; Nijsen, MJMA; Meert, T; Van Wauwe, J; Aerssens, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：547-552 , 文章类型： Article，,卷期：2012年22-1]
- In a previous communication, the SAR of a series of potent and selective 5-sulfonyl-benzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their po...
- Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold
[作者：He, XH; Wang, LL; Zheng, ZB; Xiao, JH; Zhong, W; Li, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：553-557 , 文章类型： Article，,卷期：2012年22-1]
- A series of oxazolidin-2-one-4-carboxylic amide compounds (1a-f) were designed and synthesized as the non-phosphate S1P1 receptor agonists. The single crystal of 1e was prepared and solved to elucidate the structure of 1...
- Mitochondrial targeting of a cationic amphiphilic polyproline helix
[作者：Kalafut, D; Anderson, TN; Chmielewski, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：561-563 , 文章类型： Article，,卷期：2012年22-1]
- The development of cell penetrating peptides (CPPs) for the cellular delivery of attached cargo is an area of growing interest. Many CPPs, however, are found trapped within endosomes, thereby limiting their use as drug d...
- Synthesis of [C-11]uric acid, using [C-11]phosgene, as a possible biomarker in PET imaging for diagnosis of gout
[作者：Yashio, K; Katayama, Y; Takashima, T; Ishiguro, N; Doi, H; Suzuki, M; Wada, Y; Tamai, I; Watanabe, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：115-119 , 文章类型： Article，,卷期：2012年22-1]
- The synthesis and in vivo evaluation of C-11 -labeled uric acid ([C-11]1), a potential imaging agent for the diagnosis of urate-related life-style diseases, was performed using positron emission tomography (PET) image an...
- Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists
[作者：Sundar, BG; Bailey, TR; Dunn, DD; Bacon, ER; Salvino, JM; Morton, GC; Aimone, LD; Huang, ZQ; Mathiasen, JR; Dicamillo, A; Huffman, MJ; McKenna, BA; Kopec, K; Lu, LD; Brown, R; Qian, J; Angeles, T; Connors, T; Spais, C; Holskin, B; Galinis, D; Duzic, E; Schaffhauser, H; Rosse, GC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：120-123 , 文章类型： Article，,卷期：2012年22-1]
- 7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, bra...
- Detection of single nucleotide polymorphisms within a sequence of a gene associated with prostate cancer using a fluorophore-tagged DNA probe
[作者：Zhao, ZY; San, M; Duprey, JLHA; Arrand, JR; Vyle, JS; Tucker, JHR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：129-132 , 文章类型： Article，,卷期：2012年22-1]
- Single nucleotide polymorphisms within a sequence of a gene associated with prostate cancer were identified using oligodeoxynucleotide probe sequences bearing internal anthracene fluorophores proximal to the SNP site. De...
- Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases
[作者：Zificsak, CA; Gingrich, DE; Breslin, HJ; Dunn, DD; Milkiewicz, KL; Theroff, JP; Thieu, TV; Underiner, TL; Weinberg, LR; Aimone, LD; Albom, MS; Mason, JL; Saville, L; Husten, J; Angeles, TS; Finn, JP; Jan, M; O'Kane, TM; Dobrzanski, P; Dorsey, BD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：133-137 , 文章类型： Article，,卷期：2012年22-1]
- The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression. (C) 2011 Elsevier Ltd. All...
- An iminosugar N-pentafluorobenzyl-1-deoxynojirimycin as a novel potential immunosuppressant for the treatment of Th2-related diseases
[作者：Liu, M; Wang, SR; Zhou, YD; Xiang, T; Dong, HF; Yang, K; Zhang, XL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：564-570 , 文章类型： Article，,卷期：2012年22-1]
- Increased levels of Th2 cytokine interleukin-4 (IL-4) have been reported to be involved in the pathogenesis of the parasite Schistosoma japonicum (S. japonicum) infection or detected in the serum of the causative agent o...
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