- Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester
[作者：Wang, P; Liu, C; Sanches, T; Zhong, Y; Liu, B; Xiong, JL; Neamati, N; Zhao, GS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4574-4578 , 文章类型： Article，,卷期：2009年19-16]
- A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at ...
- C-29 sterols with a cyclopropane ring at C-25 and 26 from the Vietnamese marine sponge Ianthella sp and their anticancer properties
[作者：Tung, NH; Minh, CV; Ha, TT; Kiem, PV; Huong, HT; Dat, NT; Nhiem, NX; Tai, BH; Hyun, JH; Kang, HK; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4584-4588 , 文章类型： Article，,卷期：2009年19-16]
- Two new C-29 sterols with a cyclopropane ring at C-25 and C-26, petrosterol-3,6-dione (1) and 5 alpha, 6 alpha-epoxy-petrosterol (2), along with petrosterol (3), were isolated from the Vietnamese marine sponge Ianthella ...
- Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists
[作者：Kishino, H; Moriya, M; Sakuraba, S; Sakamoto, T; Takahashi, H; Suzuki, T; Moriya, R; Ito, M; Iwaasa, H; Takenaga, N; Ishihara, A; Kanatani, A; Sato, N; Fukami, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4589-4593 , 文章类型： Article，,卷期：2009年19-16]
- A series of imidazo[1,2-a] pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a] pyridine provided compoun...
- Synthesis and biological evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives and their precursors as antileukemic agents
[作者：Gowda, NRT; Kavitha, CV; Chiruvella, KK; Joy, O; Rangappa, KS; Raghavan, SC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4594-4600 , 文章类型： Article，,卷期：2009年19-16]
- We report here the synthesis and preliminary evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives 6(a-k) and their precursors 5(a-k) as potential chemotherapeutic agents. In each case...
- Isoplatensimycin: Synthesis and biological evaluation
[作者：Jang, KP; Kim, CH; Na, SW; Kim, H; Kang, H; Lee, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4601-4602 , 文章类型： Article，,卷期：2009年19-16]
- Isoplatensimycin, a novel analog of platensimycin, was synthesized via intramolecular dipolar cycloaddition of a carbonyl ylide. Isoplatensimycin showed little activities against strains of Staphylococcus aureus, but exh...
- Synthesis and opioid receptor activity of indolopropellanes
[作者：Li, FY; Gaob, LH; Yin, CL; Chen, J; Liu, JG; Xie, X; Zhang, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4603-4606 , 文章类型： Article，,卷期：2009年19-16]
- A series of skeletal rearranged indolomorphinans 7a-d were obtained by N-demethylation of 3-methoxy-N-methyl-14-hydroxymorphinan-6-one 12 followed by N-realkylation, reduction and Fischer indole cyclization. The structur...
- Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: Part 1
[作者：Nakao, A; Ohkawa, N; Nagasaki, T; Kagari, T; Doi, H; Shimozato, T; Ushiyama, S; Aoki, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4607-4610 , 文章类型： Article，,卷期：2009年19-16]
- We investigated proinflammatory cytokine TNF alpha production inhibitors in order to develop novel anti-inflammatory agents. According to the results, we found that 17, a pyrrole derivative possessing a tetrahydropyridin...
- Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: Exploration and optimization of alternative pyrazole structure
[作者：Sugimoto, Y; Kobayashi, K; Asai, M; Ohno, A; Yamada, K; Ozaki, S; Ohta, H; Okamoto, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4611-4616 , 文章类型： Article，,卷期：2009年19-16]
- Nonpeptidic small-molecule NOP/ORL1 receptor antagonists with an imidazole scaffold were designed and synthesized to investigate alternatives to the pyrazole analog. Systematic modification of the original pyrazole lead ...
- Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: Improving cell based activity by the quaternarization of a chiral center
[作者：Nizi, E; Orsale, MV; Crescenzi, B; Pescatore, G; Muraglia, E; Alfieri, A; Gardelli, C; Spieser, SAH; Summa, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4617-4621 , 文章类型： Article，,卷期：2009年19-16]
- In the context of HIV-integrase, dihydroxypyrimidine and N-methyl pyrimidone inhibitors the cellular activity of this class of compounds has been optimized by the introduction of a simple methyl substituent in the alpha-...
- Design of selective Cathepsin inhibitors
[作者：Bethel, PA; Gerhardt, S; Jones, EV; Kenny, PW; Karoutchi, GI; Morley, AD; Oldham, K; Rankine, N; Augustin, M; Krapp, S; Simader, H; Steinbacher, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4622-4625 , 文章类型： Article，,卷期：2009年19-16]
- A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.
- Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors
[作者：Lucas, MC; Carter, DS; Cai, HY; Lee, EK; Schoenfeld, RC; Steiner, S; Villa, M; Weikert, RJ; Iyer, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4630-4633 , 文章类型： Article，,卷期：2009年19-16]
- A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibit...
- Discovery of a novel protein kinase B inhibitor by structure-based virtual screening
[作者：Medina-Franco, JL; Giulianotti, MA; Yu, YP; Shen, LL; Yao, LB; Singh, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4634-4638 , 文章类型： Article，,卷期：2009年19-16]
- Protein kinase B (PKB/AKT) is a promising and attractive therapeutic target in anticancer drug development. Herein, we report the findings of virtual screening for novel ATP-competitive inhibitors of AKT-2 using 2D- and ...
- Discovery of CYT997: a structurally novel orally active microtubule targeting agent
[作者：Burns, CJ; Harte, MF; Bu, XY; Fantino, E; Joffe, M; Sikanyika, H; Su, S; Tranberg, CE; Wilson, N; Charman, SA; Shackleford, DM; Wilks, AF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4639-4642 , 文章类型： Article，,卷期：2009年19-16]
- CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds l...
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