- Radiosynthesis of three [(11)C]ureido-substituted benzenesulfonamides as PET probes for carbonic anhydrase IX in tumors
[作者:Asakawa, C; Ogawa, M; Kumata, K; Fujinaga, M; Yamasaki, T; Xie, L; Yui, J; Kawamura, K; Fukumura, T; Zhang, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7017-7020 , 文章类型: Article,,卷期:2011年21-23]
- Three ureido-substituted benzenesulfonamides 1a-c have been developed as potent inhibitors for carbonic anhydrase IX, which is overexpressed in hypoxic tumors. In this study, we labeled these unsymmetrical ureas 1a-c usi...
- Substrate profiling of IGF-1R and InsR: Identification of a potent pentamer substrate
[作者:Chapelat, J; Berst, F; Marzinzik, AL; Moebitz, H; Drueckes, P; Fabbro, D; Trappe, J; Seebach, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7030-7033 , 文章类型: Article,,卷期:2011年21-23]
- Protein kinases are widely recognized as important therapeutic targets due to their involvement in signal transduction pathways. These pathways are tightly controlled and regulated, notably by the ability of kinases to s...
- Synthesis of novel 3-carboxamide-benzocoumarin derivatives as orally active antithrombotic agents
[作者:Sashidhara, KV; Kumar, A; Kumar, M; Singh, S; Jain, M; Dikshit, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7034-7040 , 文章类型: Article,,卷期:2011年21-23]
- In an effort to develop potent antithrombotic agents, a series of novel 3-carboxamide-benzocoumarin derivatives were synthesized and screened for their in vivo antithrombotic activity. Among 20 compounds tested, the comp...
- Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases
[作者:Casu, L; Cottiglia, F; Leonti, M; De Logu, A; Agus, E; Tse-Dinh, YC; Lombardo, V; Sissi, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7041-7044 , 文章类型: Article,,卷期:2011年21-23]
- From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and ant...
- TACN-containing cationic lipids with ester bond: Preparation and application in gene delivery
[作者:Zhang, QF; Yang, WH; Yi, WJ; Zhang, J; Ren, J; Luo, TY; Zhu, W; Yu, XQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7045-7049 , 文章类型: Article,,卷期:2011年21-23]
- A series of novel cationic lipids based on 1,4,7-triazacyclononane (TACN) with different hydrophobic chains were synthesized via the formation of a biodegradable ester bond. These lipids were found to have good buffering...
- Discovery of small molecules that enhance astrocyte differentiation in rat fetal neural stem cells
[作者:Chang, DJ; Jeong, MY; Song, J; Jin, CY; Suh, YG; Kim, HJ; Min, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7050-7053 , 文章类型: Article,,卷期:2011年21-23]
- 1,3,4-Oxadiazole derivatives were found to enhance astrocyte differentiation in rat fetal neural stem cells (NSCs). Differentiation activity was assessed by immunocytochemistry and analysis of mRNA expression of astrocyt...
- Synthesis and cytotoxic evaluation of novel paraconic acid analogs
[作者:Le Floch, C; Le Gall, E; Leonel, E; Martens, T; Cresteil, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7054-7058 , 文章类型: Article,,卷期:2011年21-23]
- A novel class of 2,3-tri- and tetrasubstituted gamma-butyrolactones analogous to paraconic acids has been synthesized in one step using a straightforward three-component reaction among aryl bromides, dimethyl itaconate a...
- Anisotropy studies of tRNA-T box antiterminator RNA complex in the presence of 1,4-disubstituted 1,2,3-triazoles
[作者:Zhou, S; Acquaah-Harrison, G; Bergmeier, SC; Hines, JV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7059-7063 , 文章类型: Article,,卷期:2011年21-23]
- The binding of tRNA to the T box antiterminator RNA element is a critical component of the T box riboswitch mechanism that regulates essential genes in many Gram-positive bacteria. A series of 1,4-disubstituted 1,2,3-tri...
- Novel inhibitors of Mycobacterium tuberculosis dTDP-6-deoxy-L-lyxo-4-hexulose reductase (RmlD) identified by virtual screening
[作者:Wang, Y; Hess, TN; Jones, V; Zhou, JZ; McNeil, MR; McCammon, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7064-7067 , 文章类型: Article,,卷期:2011年21-23]
- The complex and highly impermeable cell wall of Mycobacterium tuberculosis (Mtb) is largely responsible for the ability of the mycobacterium to resist the action of chemical therapeutics. An L-rhamnosyl residue, which oc...
- A small molecule that preferentially binds the closed conformation of Hsp90
[作者:Alexander, LD; Partridge, JR; Agard, DA; McAlpine, SR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7068-7071 , 文章类型: Article,,卷期:2011年21-23]
- Described is the synthesis of three different fluorescein-tagged derivatives of a macrocycle, and their binding affinity to heat shock protein 90 (Hsp90). Using fluorescence polarization anisotropy, we report the binding...
- Synthesis and SAR of 2-Phenoxypyridines as novel c-Jun N-terminal kinase inhibitors
[作者:Song, XY; Chen, WM; Lin, L; Ruiz, CH; Cameron, MD; Duckett, DR; Kamenecka, TM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7072-7075 , 文章类型: Article,,卷期:2011年21-23]
- The design and synthesis of a novel series of c-jun N-terminal kinase (JNK3) inhibitors is described. The development and optimization of the 2-phenoxypyridine series was carried out from an earlier pyrimidine series of ...
- Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H(3) receptor antagonists
[作者:Becknell, NC; Lyons, JA; Aimone, LD; Gruner, JA; Mathiasen, JR; Raddatz, R; Hudkins, RL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7076-7080 , 文章类型: Article,,卷期:2011年21-23]
- 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl) propoxy]-phenyl}-2H-pyridazin-3-one 6 (Irdabisant; CEP-26401) was recently reported as a potent H(3)R antagonist with excellent drug-like properties and in vivo activity that advanced...
- The synthesis of xanthones, xanthenediones, and spirobenzofurans: Their antibacterial and antifungal activity
[作者:Omolo, JJ; Johnson, MM; van Vuuren, SF; de Koning, CB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7085-7088 , 文章类型: Article,,卷期:2011年21-23]
- Exposure of the phenol, (5-bromo-2-hydroxyphenyl)(2,4,5-trimethoxyphenyl)methanone 18 to ceric ammonium nitrate (CAN) resulted in the formation of 7-bromo-3,4a-dimethoxy-2H-xanthene-2,9( 4aH)-dione 19 and 5-bromo-2',5'-d...
|