- Synthesis and evaluation of cytotoxic effects of novel alpha-methylenelactone tetracyclic diterpenoids
[作者：Zeng, YF; Wu, JQ; Shi, LY; Wang, K; Zhou, B; Tang, Y; Zhang, DY; Wu, YC; Hua, WY; Wu, XM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1922-1925 , 文章类型： Article，,卷期：2012年22-5]
- A series of tetracyclic diterpenoids bearing the alpha-methylenelactone group have been synthesized and screened for their in vitro anti-tumor activities against six human cancer cell lines. The results showed that compo...
- Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl) benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain
[作者：Hirata, Y; Hirata, M; Kawaratani, Y; Shibano, M; Taniguchi, M; Yasuda, M; Ohmomob, Y; Nagaoka, Y; Baba, K; Uesato, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1926-1930 , 文章类型： Article，,卷期：2012年22-5]
- New orally bioavailable 5-(thiophen-2-yl)-substituted 2-aminobenzamide-series histone deacetylase inhibitors were synthesized. These compounds possess a morpholine or piperadine-derived moiety as an aqueous soluble funct...
- Influence of ring size on the cognition-enhancing activity of DM235 and MN19, two potent nootropic drugs
[作者：Guandalini, L; Martini, E; Mannelli, LD; Dei, S; Manetti, D; Scapecchi, S; Teodori, E; Ghelardini, C; Romanelli, MN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1936-1939 , 文章类型： Article，,卷期：2012年22-5]
- A series of analogs of DM235 and MN19, characterized by rings with different size, have been prepared and evaluated for their nootropic activity in the mouse passive-avoidance test. It was found that the optimal ring siz...
- Aminopyrimidinone Cdc7 Kinase Inhibitors
[作者：Woods, KW; Lai, CQ; Miyashiro, JM; Tong, YS; Florjancic, AS; Han, EK; Soni, N; Shi, Y; Lasko, L; Leverson, JD; Johnson, EF; Shoemaker, AR; Penning, TD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1940-1943 , 文章类型： Article，,卷期：2012年22-5]
- We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (K-i) less than 1 nM. Kinase selectivity is reasonable...
- Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors
[作者：Bauer, U; Giordanetto, F; Bauer, M; O'Mahony, G; Johansson, KE; Knecht, W; Hartleib-Geschwindner, J; Carlsson, ET; Enroth, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1944-1948 , 文章类型： Article，,卷期：2012年22-5]
- A series of 1,6-naphthyridine-based compounds was synthesized as potent phosphodiesterase 10A (PDE10A) inhibitors. Structure-based chemical modifications of the discovered chemotype served to further improve potency and ...
- Novel bisbenzimide-nitroxides for nuclear redox imaging in living cells
[作者：Ikeda, M; Nakagawa, H; Suzuki, T; Miyata, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1949-1952 , 文章类型： Article，,卷期：2012年22-5]
- Nuclear oxidative stress damages genomic DNA and may lead to cell death, leading to aging and aging-related disorders. Though it is important to measure the nuclear oxidative stress separately, there are still little exa...
- 3,4-Diarylpiperidines as potent renin inhibitors
[作者：Lacombe, P; Arbour, M; Aspiotis, R; Cauchon, E; Chen, A; Dube, D; Falgueyret, JP; Fournier, PA; Gallant, M; Grimm, E; Han, YX; Juteau, H; Liu, S; Mellon, C; Ramtohul, Y; Simard, D; St-Jacques, R; Tsui, GC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1953-1957 , 文章类型： Article，,卷期：2012年22-5]
- The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC50, had a clean CYP 3A4 p...
- Novel substituted 9-norbornylpurines and their activities against RNA viruses
[作者：Sala, M; Hrebabecky, H; Leyssen, P; Dejmek, M; Dracinsky, M; De Palma, AM; Neyts, J; Nencka, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1963-1968 , 文章类型： Article，,卷期：2012年22-5]
- We report on the synthesis and the study of the structure-activity relationship of novel 9-norbornyl-6-chloropurine derivatives, which exert selective antiviral activity on the replication of Coxsackievirus B3. In partic...
- SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase
[作者：Hieke, M; Rodl, CB; Wisniewska, JM; la Buscato, E; Stark, H; Schubert-Zsilavecz, M; Steinhilber, D; Hofmann, B; Proschak, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1969-1975 , 文章类型： Article，,卷期：2012年22-5]
- A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a] pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening...
- Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors
[作者：Yan, JW; Huang, N; Li, SK; Yang, LM; Xing, WQ; Zheng, YT; Hu, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1976-1979 , 文章类型： Article，,卷期：2012年22-5]
- A series of P1-substituted biaryl amprenavir derivatives was designed and synthesized. These compounds were evaluated for enzyme inhibition and antiviral activity in vitro. Several compounds showed highly efficient antiv...
- 3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors
[作者：Annedi, SC; Maddaford, SP; Ramnauth, J; Renton, P; Speed, J; Rakhit, S; Andrews, JS; Porreca, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1980-1984 , 文章类型： Article，,卷期：2012年22-5]
- A series of 3,5-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS). Various guanidine isosteric groups were explored at the 5-position of the indol...
- Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH
[作者：Kirubakaran, S; Gorla, SK; Sharling, L; Zhang, MJ; Liu, XP; Ray, SS; MacPherson, IS; Striepen, B; Hedstrom, L; Cuny, GD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1985-1988 , 文章类型： Article，,卷期：2012年22-5]
- Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5...
- 5-Aryl-4-carboxamide-1,3-oxazoles: Potent and selective GSK-3 inhibitors
[作者：Gentile, G; Merlo, G; Pozzan, A; Bernasconi, G; Bax, B; Bamborough, P; Bridges, A; Carter, P; Neu, M; Yao, G; Brough, C; Cutler, G; Coffin, A; Belyanskaya, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1989-1994 , 文章类型： Article，,卷期：2012年22-5]
- 5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described. Crown Copyright (C...
- A domino Knoevenagel hetero-Diels-Alder reaction for the synthesis of polycyclic chromene derivatives and evaluation of their cytotoxicity
[作者：Reddy, BVS; Divya, B; Swain, M; Rao, TP; Yadav, JS; Vardhan, MVPSV,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1995-1999 , 文章类型： Article，,卷期：2012年22-5]
- A novel octahydrochromeno[4,3-a]xanthen-1(2H)-one derivatives has been prepared using 10 mol % DL-proline in ethanol via a domino Knoevenagel hetero-Diels-Alder reaction of alkene-tethered chromene-3-carboxaldehyde with ...
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