- In vitro biological evaluation of novel 7-O-dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines
[作者：Bonesi, M; Tundis, R; Deguin, B; Loizzo, MR; Menichini, F; Tillequin, F; Menichini, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5431-5434 , 文章类型： Article，,卷期：2008年18-20]
- The effect of novel pectolinarigenin derivatives bearing a dialkylaminoalkyl substituent at O-7 on cell proliferation was evaluated in vitro in a panel of seven human cancer cell lines including renal adenocarcinoma ACHN...
- (3R)-3-amino-4-(2,4,5-trigluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamideas a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
[作者：Nitta, A; Fujii, H; Sakami, S; Nishimura, Y; Ohyama, T; Satoh, M; Nakaki, J; Satoh, S; Inada, C; Kozono, H; Kumagai, H; Shimamura, M; Fukazawa, T; Kawai, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5435-5438 , 文章类型： Article，,卷期：2008年18-20]
- Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides and 3-amino-N-(4-aryltetrahydropyran-4-yl)butanamides were synthesized and evaluated as dipeptidyl peptidase IV (DPP-IV) inhibitors. Derivatives incorpora...
- Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas - The effect of capping the distal basic piperidine nitrogen
[作者：Miller, NR; Daniels, RN; Bridges, TM; Brady, AE; Conn, PJ; Lindsley, CW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5443-5447 , 文章类型： Article，,卷期：2008年18-20]
- This letter describes the further synthesis and SAR, developed through an iterative analog library approach, of analogs of the highly selective M1 allosteric agonist TBPB by deletion of the distal basic piperidine nitrog...
- Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead
[作者：Carlton, DL; Collin-Smith, LJ; Daniels, AJ; Deaton, DN; Goetz, AS; Laudeman, CP; Littleton, TR; Musso, DL; Morgan, RJO; Szewczyk, JR; Zhang, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5451-5455 , 文章类型： Article，,卷期：2008年18-20]
- Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modi. cation of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery o...
- 'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors
[作者：Montalban, AG; Boman, E; Chang, CD; Ceide, SC; Dahl, R; Dalesandro, D; Delaet, NGJ; Erb, E; Gibbs, A; Kahl, J; Kessler, L; Lundstrom, J; Miller, S; Nakanishi, H; Roberts, E; Saiah, E; Sullivan, R; Wang, ZJ; Larson, CJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5456-5459 , 文章类型： Article，,卷期：2008年18-20]
- We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more ch...
- Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties
[作者：Bridges, TM; Brady, AE; Kennedy, JP; Daniels, RN; Miller, NR; Kim, K; Breininger, ML; Gentry, PR; Brogan, JT; Jones, CK; Conn, PJ; Lindsley, CW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5439-5442 , 文章类型： Article，,卷期：2008年18-20]
- This Letter describes the first account of the synthesis and SAR, developed through an iterative analogue library approach, of analogues of the highly selective M1 allosteric agonist TBPB. With slight structural changes,...
- 2,4(5)-Diarylimidazoles: Synthesis and biological evaluation of a new class of sodium channel blockers against hNa(v)1.2
[作者：Rivara, M; Baheti, AR; Fantini, M; Cocconcelli, G; Ghiron, C; Kalmar, CL; Singh, N; Merrick, EC; Patel, MK; Zuliani, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5460-5462 , 文章类型： Article，,卷期：2008年18-20]
- A small family of novel 2,4(5)-diarylimidazoles were prepared through a simple and efficient synthesis and evaluated as potential inhibitors of hNa(v)1.2 sodium channel currents. One member of this series (4) exhibited p...
- Novel and orally active 5-(1,3,4-oxadiazol-2-yl)pyrimidine derivatives as selective FLT3 inhibitors
[作者：Ishida, H; Isami, S; Matsumura, T; Umehara, H; Yamashita, Y; Kajita, J; Fuse, E; Kiyoi, H; Naoe, T; Akinaga, S; Shiotsu, Y; Arai, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5472-5477 , 文章类型： Article，,卷期：2008年18-20]
- 5-(1,3,4-Oxadiazol-2-yl)pyrimidine derivative 1 was identified as a new class of FLT3 inhibitor from our compound library. With the aim of enhancement of antitumor activity of 2 prepared by minor modi. cation of1, struct...
- Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas
[作者：Jin, J; Wang, YH; Shi, DC; Wang, F; Fu, W; Davis, RS; Jin, Q; Foley, JJ; Sarau, HM; Morrow, DM; Moore, ML; Rivero, RA; Palovich, M; Salmon, M; Belmonte, KE; Busch-Petersen, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5481-5486 , 文章类型： Article，,卷期：2008年18-20]
- SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M-3 over M-1. The struc...
- Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors
[作者：Anderson, M; Andrews, DM; Barker, AJ; Brassington, CA; Breed, J; Byth, KF; Culshaw, JD; Finlay, MRV; Fisher, E; McMiken, HHJ; Green, CP; Heaton, DW; Nash, IA; Newcombe, NJ; Oakes, SE; Pauptit, RA; Roberts, A; Stanway, JJ; Thomas, AP; Tucker, JA; Walker, M; Weir, HM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5487-5492 , 文章类型： Article，,卷期：2008年18-20]
- An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been developed. Protein inhibitor structure determination has provided an understanding of the emerging structure activity trends for the imidazole seri...
- 3-(Imidazolylmethyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators
[作者：Zhang, L; Rogers, BN; Duplantier, AJ; McHardy, SF; Efremov, I; Berke, H; Qian, WM; Zhang, AQ; Maklad, N; Candler, J; Doran, AC; Lazzaro, JT; Ganong, AH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5493-5496 , 文章类型： Article，,卷期：2008年18-20]
- The synthesis and structure-activity relationship (SAR) of a novel series of 3-(imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers, derived from a high throughput screening (HTS), are described. Subsequent o...
- Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: Virtual screening, synthesis, and biological evaluation
[作者：Deng, GH; Li, WH; Shen, JH; Jiang, HL; Chen, KX; Liu, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5497-5502 , 文章类型： Article，,卷期：2008年18-20]
- The identification of a novel pyrazolidine-3,5-dione based scaffold hit compound as Farnesoid X receptor (FXR) partial or full agonist has been accomplished by means of virtual screening techniques. A series of pyrazolid...
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