- Synthesis and evaluation of piperazine and homopiperazine analogues of JS-K, an anti-cancer lead compound
[作者：Nandurdikar, RS; Maciag, AE; Citro, ML; Shami, PJ; Keefer, LK; Saavedra, JE; Chakrapani, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2760-2762 , 文章类型： Article，,卷期：2009年19-10]
- Here we report a number of novel JS-K structural analogues with sub-micromolar anti-proliferative activities against human leukemia cell lines HL-60 and U937; JS-K is the anti-cancer lead compound O-2-(2,4-dinitrophenyl)...
- Low molecular weight non-peptide mimics of omega-conotoxin GVIA
[作者：Duggan, PJ; Lewis, RJ; Lok, YP; Lumsden, NG; Tuck, KL; Yang, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2763-2765 , 文章类型： Article，,卷期：2009年19-10]
- We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide omega-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193 g/mol compared...
- Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H-1 antagonists
[作者：Kubota, K; Kurebayashi, H; Miyachi, H; Tobe, M; Onishi, M; Isobe, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2766-2771 , 文章类型： Article，,卷期：2009年19-10]
- A series of phenothiazine carboxylic acid derivatives, having 6-amino-pyrimidine-2,4(1H,3H)-dione moiety via a appropriate linker, were synthesized and evaluated for their affinity toward human histamine H-1 receptor and...
- Synthesis and biological activities of a pH-dependently activated water-soluble prodrug of a novel hexacyclic camptothecin analog
[作者：Ohwada, J; Ozawa, S; Kohchi, M; Fukuda, H; Murasaki, C; Suda, H; Murata, T; Niizuma, S; Tsukazaki, M; Ori, K; Yoshinari, K; Itezono, Y; Endo, M; Ura, M; Tanimura, H; Miyazaki, Y; Kawashima, A; Nagao, S; Namba, E; Ogawa, K; Kobayashi, K; Okabe, H; Umeda, I; Shimma, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2772-2776 , 文章类型： Article，,卷期：2009年19-10]
- CH0793076 (1) is a novel hexacyclic camptothecin analog showing potent antitumor activity in various human caner xenograft models. To improve the water solubility of 1, water-soluble prodrugs were designed to generate an...
- 2-Phenylquinazolin-4(3H)-one, a class of potent PDE5 inhibitors with high selectivity versus PDE6
[作者：Duan, HL; Zheng, J; Lai, QL; Liu, Z; Tian, GH; Wang, Z; Li, JF; Shen, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2777-2779 , 文章类型： Article，,卷期：2009年19-10]
- In our efforts to minimize the side effects associated with low selectivity against the other PDE isozymes, a novel class of 2-phenylquinazolin-4(3H)-one derivatives were designed and prepared as potent PDE5 inhibitors w...
- Discovery of 4-azaindoles as novel inhibitors of c-Met kinase
[作者：Porter, J; Lumb, S; Franklin, RJ; Gascon-Simorte, JM; Calmiano, M; Le Riche, K; Lallemand, B; Keyaerts, J; Edwards, H; Maloney, A; Delgado, J; King, L; Foley, A; Lecomte, F; Reuberson, J; Meier, C; Batchelor, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2780-2784 , 文章类型： Article，,卷期：2009年19-10]
- A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future direct...
- Synthesis of novel nitric oxide (NO)-releasing esters of timolol
[作者：Chiroli, V; Batugo, MR; Biondi, S; Bonfanti, A; Brambilla, S; Gale, DC; Li, L; Miglietta, D; Nicoli, F; Prasanna, GA; Ronchetti, D; Vernier, WF; Chong, WKM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2785-2788 , 文章类型： Article，,卷期：2009年19-10]
- A novel class of timolol derivatives with nitric oxide (NO)-donating moieties achieved chemical stability yet under physiologically relevant conditions released timolol and NO. Hindered esters A were designed and synthes...
- Novel zinc finger nuclease created by combining the Cys(2)His(2)- and His(4)-type zinc finger domains
[作者：Negi, S; Umeda, Y; Masuyama, S; Kano, K; Sugiura, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2789-2791 , 文章类型： Article，,卷期：2009年19-10]
- To improve the DNA hydrolytic activity of the zinc finger nuclease, we have created a new artificial zinc finger nuclease (ZWH4) by connecting two distinct zinc finger domains possessing different types of Zn(II) binding...
- Design and synthesis of novel delta opioid receptor agonists and their pharmacologies
[作者：Nagase, H; Osa, Y; Nemoto, T; Fujii, H; Imai, M; Nakamura, T; Kanemasa, T; Kato, A; Gouda, H; Hirono, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2792-2795 , 文章类型： Article，,卷期：2009年19-10]
- We re-examined the accessory site of the 4,5-epoxymorphinan skeleton by CAMDAS conformational analysis in an effort to deign novel delta opioid receptor antagonists. We synthesized three novel compounds (SN-11, 23 and 28...
- Synthesis and cytotoxicities of icogenin analogues with disaccharide residues
[作者：Wang, HX; Su, FQ; Zhou, L; Chen, XG; Lei, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2796-2800 , 文章类型： Article，,卷期：2009年19-10]
- For further structure-activity relationships (SAR) research of furostan saponin, two icogenin analogues: (25R)-22-O-methyl-furost-5-en-3 beta, 26-diol-3-O-alpha-L-rhamnopyranosyl-(1 -> 2)-beta-D-glucopyranoside 1 and (25...
- Protein tyrosine phosphatase 1B inhibitory effects of depsidone and pseudodepsidone metabolites from the Antarctic lichen Stereocaulon alpinum
[作者：Seo, C; Sohn, JH; Ahn, JS; Yim, JH; Lee, HK; Oh, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2801-2803 , 文章类型： Article，,卷期：2009年19-10]
- Seven phenolic lichen metabolites (1-7) have been isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum by various chromatographic methods. The structures of these compounds were determined mainly...
- Synthesis and characterization of a BODIPY-labeled derivative of Soraphen A that binds to acetyl-CoA carboxylase
[作者：Raymer, B; Kavana, M; Price, A; Wang, B; Corcoran, L; Kulathila, R; Groarke, J; Mann, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2804-2807 , 文章类型： Article，,卷期：2009年19-10]
- BODIPY-labeled Soraphen A derivative 4 was synthesized and characterized as an acetyl-CoA carboxylase (ACC) binder. Biophysical measurements indicate that the molecule binds in the biotin carboxylase domain where Soraphe...
- Synthesis and evaluation of carbamate prodrugs of SQ109 as antituberculosis agents
[作者：Meng, QY; Luo, HB; Liu, YB; Li, W; Zhang, W; Yao, QZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2808-2810 , 文章类型： Article，,卷期：2009年19-10]
- The low bioavailability of SQ109 in rats, resulting from first-pass effect in the liver, may be remedied by prodrug strategy. Based on esterase-sensitive carbamate prodrug strategy, a novel series of prodrugs of SQ109 ha...
- Design, synthesis, and characterization of 6 beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes
[作者：Pelotte, AL; Smith, RM; Ayestas, M; Dersch, CM; Bilsky, EJ; Rothman, RB; Deveau, AM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2811-2814 , 文章类型： Article，,卷期：2009年19-10]
- Since the mu opioid receptor (MOR) is known to be involved in the therapeutically relevant pathways leading to the manifestation of pain and addiction, we are currently studying the specific structural characteristics th...
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