- Preparation and antibacterial evaluation of decarboxylated fluoroquinolones
[作者:Nguyen, ST; Ding, XY; Butler, MM; Tashjian, TF; Peet, NP; Bowlin, TL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5961-5963 , 文章类型: Article,,卷期:2011年21-19]
- Decarboxylated ciprofloxacin (3) has been reported in the literature to have antibacterial activities against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Bacillus subtilis, Enterobacter cloa...
- 3D QSAR and docking study of flavone derivatives as potent inhibitors of influenza H1N1 virus neuraminidase
[作者:Gao, L; Zu, M; Wu, S; Liu, AL; Du, GH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5964-5970 , 文章类型: Article,,卷期:2011年21-19]
- Although several flavonoids have been reported to exert inhibitory effects on influenza H1N1 neuraminidase (NA), little is known about the structure-activity relationship and binding mode. Three dimensional QSAR (quantit...
- RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor
[作者:Krysko, AA; Samoylenko, GV; Polishchuk, PG; Andronati, SA; Kabanova, TA; Khristova, TM; Kuz'min, VE; Kabanov, VM; Krysko, OL; Varnek, AA; Grygorash, RY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5971-5974 , 文章类型: Article,,卷期:2011年21-19]
- The novel RGD mimetics with phthalimidine central fragment were synthesized with the use of 4-piperidine-4-yl-butyric, 4-piperidine-4-yl-butyric, 4-piperazine-4-yl-benzoic and 1,2,3,4-tetrahydroiso-quinoline-7-carboxylic...
- Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d] pyrimidines
[作者:Mo, WY; Liang, YJ; Gu, YC; Fu, LW; He, HW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5975-5977 , 文章类型: Article,,卷期:2011年21-19]
- Synthesis and cytotoxicity of 11 4-methylene pyrido[4,3-d] pyrimidines 5a-k were described. Cytotoxicity assay results showed that some compounds had much stronger antitumor activity than Fluorouracil against KB cell lin...
- Synthesis of phenanthroindolizidine alkaloids and evaluation of their antitumor activities and toxicities
[作者:Ikeda, T; Yaegashi, T; Matsuzaki, T; Yamazaki, R; Hashimoto, S; Sawada, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5978-5981 , 文章类型: Article,,卷期:2011年21-19]
- We previously reported that phenanthroindolizidine alkaloid 3 and its derivatives had markedly potent in vitro cytotoxicity. However, they had low in vivo antitumor activities and high in vivo toxicities, which was a ser...
- Formation, recognition and bioactivities of a novel G-quadruplex in the STAT3 gene
[作者:Lin, S; Li, SF; Chen, Z; He, XW; Zhang, YY; Xu, XJ; Xu, M; Yuan, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5987-5991 , 文章类型: Article,,卷期:2011年21-19]
- G-Quadruplexes have been proved to exist in 5'-untranslated region (5'-UTR), promoter, intron and exon regions of many human genes. Here we report an intramolecular G-quadruplex formed by a G-rich sequence in the 3'-flan...
- Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors
[作者:Sleebs, BE; Nikolakopoulos, G; Street, IP; Falk, H; Baell, JB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5992-5994 , 文章类型: Article,,卷期:2011年21-19]
- 4-Aminobenzothieno[3,2-d]pyrimidines were previously identified in a high throughput screening campaign as LIMK1 inhibitors. Scaffold reversal led to the identification of a series of simple 5,6-substituted 4-aminothieno...
- 4-Thiophenoxy-2-trichloromethyquinazolines display in vitro selective antiplasmodial activity against the human malaria parasite Plasmodium falciparum
[作者:Verhaeghe, P; Dumetre, A; Castera-Ducros, C; Hutter, S; Laget, M; Fersing, C; Prieri, M; Yzombard, J; Sifredi, F; Rault, S; Rathelot, P; Vanelle, P; Azas, N,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6003-6006 , 文章类型: Article,,卷期:2011年21-19]
- A series of original quinazolines bearing a 4-thiophenoxy and a 2-trichloromethyl group was synthesized in a convenient and efficient way and was evaluated toward its in vitro antiplasmodial potential. The series reveale...
- Dual pro-drugs of 2 '-C-methyl guanosine monophosphate as potent and selective inhibitors of hepatitis C virus
[作者:McGuigan, C; Madela, K; Aljarah, M; Gilles, A; Battina, SK; Ramamurty, CVS; Rao, CS; Vernachio, J; Hutchins, J; Hall, A; Kolykhalov, A; Henson, G; Chamberlain, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6007-6012 , 文章类型: Article,,卷期:2011年21-19]
- We have previously reported the power of combining a 5'-phosphoramidate ProTide, phosphate prodrug, motif with a 6-methoxy purine pro-drug entity to generate highly potent anti-HCV agents, leading to agents in clinical t...
- Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P1 agonists
[作者:Buzard, D; Han, SD; Thoresen, L; Moody, J; Lopez, L; Kawasaki, A; Schrader, T; Sage, C; Gao, YH; Edwards, J; Barden, J; Thatte, J; Fu, LX; Solomon, M; Liu, L; Al-Shamma, H; Gatlin, J; Le, M; Xing, C; Espinola, S; Jones, RM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6013-6018 , 文章类型: Article,,卷期:2011年21-19]
- S1P(1) receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P(1) receptor agonists, we have identified a nov...
- Synthesis and antihistamine evaluations of novel loratadine analogues (vol 21, pg 4454, 2011)
[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:6019-6019 , 文章类型: Correction,,卷期:2011年21-19]
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