- 4-Piperidin-4-ylidenemethyl-benzamides as delta-opioid receptor agonists for CNS indications: Identifying clinical candidates
[作者：Dantzman, CL; King, MM; Ernst, GE; Wang, X; McCauley, JP; Andisik, DW; Brush, K; Bui, KH; Frietze, W; Hoesch, V; Liu, J; Palmer, WE; Spear, N; Hudzik, TJ; Wesolowski, SS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1174-1178 , 文章类型： Article，,卷期：2012年22-2]
- A series of 4-piperidin-4-ylidenemethyl-benzamide delta-opioid receptor agonists is described with an emphasis on balancing the potency, subtype selectivity and in vitro ADME and safety properties. The three sites impact...
- Discovery of novel alpha 7 nicotinic acetylcholine receptor ligands via pharmacophoric and docking studies of benzylidene anabaseine analogs
[作者：Kombo, DC; Mazurov, AA; Chewning, J; Hammond, PS; Tallapragada, K; Hauser, TA; Speake, J; Yohannes, D; Caldwell, WS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1179-1186 , 文章类型： Article，,卷期：2012年22-2]
- Based on pharmacophore elucidation and docking studies on interactions of benzylidene anabaseine analogs with AChBPs and alpha 7 nAChR, novel spirodiazepine and spiroimidazoline quinuclidine series have been designed. Bi...
- A simple oxazolidine linker for solid-phase synthesis of peptide aldehydes
[作者：Kang, W; Wang, WG; Zhi, XX; Zhang, B; Wei, P; Xu, HY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1187-1188 , 文章类型： Article，,卷期：2012年22-2]
- A very simple and cheap linker has been used for solid-phase synthesis of peptide aldehydes. Protected amino acid aldehydes are immobilized on 2-Cl(trt) resin as oxazolidine formation via diethanolamine. After classical ...
- Discovery of novel and potent CRTH2 antagonists
[作者：Ito, S; Terasaka, T; Zenkoh, T; Matsuda, H; Hayashida, H; Nagata, H; Imamura, Y; Kobayashi, M; Takeuchi, M; Ohta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1194-1197 , 文章类型： Article，,卷期：2012年22-2]
- High throughput screening of our chemical library for CRTH2 antagonists provided a lead compound la. Initial optimization of the lead led to the discovery of a novel, potent and orally bioavailable CRTH2 antagonist 17. (...
- In vivo evaluation of oral anti-tumoral effect of 3,4-dihydroquinazoline derivative on solid tumor
[作者：Kang, HB; Rim, HK; Park, JY; Choi, HW; Choi, DL; Seo, JH; Chung, KS; Huh, G; Kim, J; Choo, DJ; Lee, KT; Lee, JY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1198-1201 , 文章类型： Article，,卷期：2012年22-2]
- An extension of our previously reported 3.4-dihydroquinazoline derivative is investigated. Oral anti-tumoral activity of 3,4-dihydroquinazoline derivative (KYS05090) as potent and selective T-type calcium channel blocker...
- Pharmacophore-based discovery of a novel cytosolic phospholipase A(2)alpha inhibitor
[作者：Noha, SM; Jazzar, B; Kuehnl, S; Rollinger, JM; Stuppner, H; Schaible, AM; Werz, O; Wolber, G; Schuster, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1202-1207 , 文章类型： Article，,卷期：2012年22-2]
- The release of arachidonic acid, a precursor in the production of prostaglandins and leukotrienes, is achieved by activity of the cytosolic phospholipase A(2)alpha (cPLA(2)alpha). Signaling mediated by this class of bioa...
- New thiazole carboxamides as potent inhibitors of Akt kinases
[作者：Chang, SH; Zhang, Z; Zhuang, XX; Luo, JF; Cao, XW; Li, HL; Tu, ZC; Lu, XY; Ren, XM; Ding, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1208-1212 , 文章类型： Article，,卷期：2012年22-2]
- A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpro...
- A multivalent approach to the discovery of long-acting beta(2)-adrenoceptor agonists for the treatment of asthma and COPD
[作者：Jacobsen, JR; Choi, SK; Combs, J; Fournier, EJL; Klein, U; Pfeiffer, JW; Thomas, GR; Yu, C; Moran, EJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1213-1218 , 文章类型： Article，,卷期：2012年22-2]
- A multivalent approach was applied to the design of long-acting inhaled beta(2)-adrenoceptor agonists. A series of dimeric arylethanolamines based on the short acting beta(2)-adrenoceptor agonist albuterol were prepared,...
- In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase
[作者：Rohe, A; Erdmann, F; Bassler, C; Wichapong, K; Sippl, W; Schmidt, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1219-1223 , 文章类型： Article，,卷期：2012年22-2]
- The human Myt1 kinase (PKMYT1) is an important regulator of the G2/M transition in the cell cycle. Presently, limited knowledge about its substrate recognition is available. Here, various potential substrates were invest...
- Identification of triazolopyridazinones as potent p38 alpha inhibitors
[作者：Herberich, B; Jackson, C; Wurz, RP; Pettus, LH; Sherman, L; Liu, QR; Henkle, B; Saris, CJM; Wong, LM; Chmait, S; Lee, MR; Mohr, C; Hsieh, F; Tasker, AS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1226-1229 , 文章类型： Article，,卷期：2012年22-2]
- Structure-activity relationship (SAR) investigations of a novel class of triazolopyridazinone p38 alpha mitogen activated protein kinase (MAPK) inhibitors are disclosed. From these studies, increased in vitro potency was...
- Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer
[作者：Guo, CX; Kephart, S; Ornelas, M; Gonzalez, J; Linton, A; Pairish, M; Nagata, A; Greasley, S; Elleraas, J; Hosea, N; Engebretsen, J; Fanjul, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1230-1236 , 文章类型： Article，,卷期：2012年22-2]
- High throughput cell-based screening led to the identification of 3-aryloxy lactams as potent androgen receptor (AR) antagonists. Refinement of these leads to improve the ADME profile and remove residual agonism led to t...
- Heteroaromatic-aminomethyl quinolones: Potent and selective iNOS inhibitors
[作者：Duron, SG; Lindstrom, A; Bonnefous, C; Zhang, H; Chen, XH; Symons, KT; Sablad, M; Rozenkrants, N; Zhang, Y; Wang, L; Yazdani, N; Shiau, AK; Noble, SA; Rix, P; Rao, TS; Hassig, CA; Smith, ND,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1237-1241 , 文章类型： Article，,卷期：2012年22-2]
- The overproduction of nitric oxide during the biological response to inflammation by the nitric oxide synthase (NOS) enzymes have been implicated in the pathology of many diseases. By removal of the amide core from uHTS-...
- Identification of novel, potent and selective inhibitors of Polo-like kinase 1
[作者：Chen, SQ; Bartkovitz, D; Cai, JP; Chen, Y; Chen, Z; Chu, XJ; Le, K; Le, NT; Luk, KC; Mischke, S; Naderi-Oboodi, G; Boylan, JF; Nevins, T; Qing, WG; Chen, YS; Wovkulich, PM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1247-1250 , 文章类型： Article，,卷期：2012年22-2]
- A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivit...
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