- Discovery of a potent and selective small molecule hGPR91 antagonist
[作者：Bhuniya, D; Umrani, D; Dave, B; Salunke, D; Kukreja, G; Gundu, J; Naykodi, M; Shaikh, NS; Shitole, P; Kurhade, S; De, S; Majumdar, S; Reddy, SB; Tambe, S; Shejul, Y; Chugh, A; Palle, VP; Mookhtiar, KA; Cully, D; Vacca, J; Chakravarty, PK; Nargund, RP; Wright, SD; Graziano, MP; Singh, SB; Roy, S; Cai, TQ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3596-3602 , 文章类型： Article，,卷期：2011年21-12]
- GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand. Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertens...
- Identification and optimisation of novel sulfonamide, selective vasopressin V(1B) receptor antagonists
[作者：Baker, J; Bingham, M; Blackburn-Munro, R; Cai, JQ; Craighead, M; Gilfillan, R; Goan, K; Jaap, D; Milne, R; Morphy, JR; Napier, S; Presland, J; Spinks, G; Thomson, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3603-3607 , 文章类型： Article，,卷期：2011年21-12]
- The synthesis and preliminary structure-activity relationships (SAR) of a novel class of vasopressin V(1B) receptor antagonists are described. Hit compound 5, identified via high throughput screening of the corporate col...
- Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor
[作者：Guerlet, G; Spangenberg, T; Mann, A; Faure, H; Ruat, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3608-3612 , 文章类型： Article，,卷期：2011年21-12]
- Desmethylveramiline (1), an aza steroid analogue of veramiline was designed as a surrogate for cyclopamine, a reference antagonist of the Sonic Hedgehog (Shh) pathway. Desmethyveramiline (1) was prepared in seven steps f...
- Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities
[作者：Xiao, QC; Liu, YQ; Qiu, YT; Yao, ZY; Zhou, GB; Yao, ZJ; Jiang, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3613-3615 , 文章类型： Article，,卷期：2011年21-12]
- A new series of linear dimeric compounds mimicking naturally occurring annonaceous acetogenins have been synthesized by bivalent analogue design, and their cytotoxicities have been evaluated against the growth of cancer ...
- Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids
[作者：Luker, T; Bonnert, R; Schmidt, J; Sargent, C; Paine, SW; Thom, S; Pairaudeau, G; Patel, A; Mohammed, R; Akam, E; Dougall, I; Davis, AM; Abbott, P; Brough, S; Millichip, I; McInally, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3616-3621 , 文章类型： Article，,卷期：2011年21-12]
- A novel series of biaryl phenoxyacetic acids was discovered as potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A hit compound 4 was discovere...
- 3-Substitued indoles: One-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities
[作者：Rao, VK; Chhikara, BS; Shirazi, AN; Tiwari, R; Parang, K; Kumar, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3511-3514 , 文章类型： Article，,卷期：2011年21-12]
- An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-me...
- alpha(v)beta(3)-Integrin-targeting lanthanide complex: Synthesis and evaluation as a tumor-homing luminescent probe
[作者：Ito, T; Inoue, M; Akamatsu, K; Kusaka, E; Tanabe, K; Nishimoto, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3515-3518 , 文章类型： Article，,卷期：2011年21-12]
- The application of lanthanide complexes in the time-resolved fluorescence imaging of living cells has emerged in the last few decades, providing high-contrast images of cells through detection of the delayed emission. In...
- Inhibition of multi-drug resistant HIV-1 reverse transcriptase by nucleoside beta-triphosphates
[作者：Dash, C; Ahmadibeni, Y; Hanley, MJ; Pandhare, J; Gotte, M; Le Grice, SFJ; Parang, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3519-3522 , 文章类型： Article，,卷期：2011年21-12]
- Despite the success of potent reverse transcriptase (RT) inhibitors against human immunodeficiency virus type 1 (HIV-1) in combination regimens, the development of drug resistant RTs constitutes a major hurdle for the lo...
- Ketonethiosemicarbazones: Structure-activity relationships for their melanogenesis inhibition
[作者：Thanigaimalai, P; Lee, KC; Sharma, VK; Roh, E; Kim, Y; Jung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3527-3530 , 文章类型： Article，,卷期：2011年21-12]
- A series of 2-(1-phenylalkylidene)hydrazinecarbothioamides 2, 2-(1-phenylalkyl) hydrazinecarbothioamides 3, 2-(3,4-dihydronaphthalen-1(2H)-ylidene) hydrazinecarbothioamide (4), and 2-(1-(thiophen-2-yl) ethylidene) hydraz...
- Synthesis, cytotoxic activities and cell cycle arrest profiles of naphtho[2,1-alpha]pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione glycosides
[作者：Ding, N; Du, XG; Zhang, W; Lu, ZC; Li, YX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3531-3535 , 文章类型： Article，,卷期：2011年21-12]
- Naphtho[2,1-alpha] pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione (NPCD) is known to be a very potent and selective cyclin D1-CDK4 inhibitors and could induce strong G1 phase arrest in breast tumor cell lines. In this work, ...
- Synthesis and evaluation of antioxidant and antibacterial activities of new substituted bis(1,3,4-oxadiazoles), 3,5-bis(substituted) pyrazoles and isoxazoles
[作者：Musad, EA; Mohamed, R; Saeed, BA; Vishwanath, BS; Rai, KML,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3536-3540 , 文章类型： Article，,卷期：2011年21-12]
- Two series of five membered heterocyclic bis(1,3,4-oxadiazole) derivatives 2(a-h) and 3,5-bis(substituted) pyrazoles, isoxazoles 3(a, b, d-i), 4(a-c) were synthesized via oxidative cyclization of some diaroylhydrazones u...
- TRPV1 modulators: Structure-activity relationships using a rational combinatorial approach
[作者：Zaccaro, L; Garcia-Lopez, MT; Gonzalez-Muniz, R; Garcia-Martinez, C; Ferrer-Montiel, A; Albericio, F; Royo, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3541-3545 , 文章类型： Article，,卷期：2011年21-12]
- A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivit...
- Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone
[作者：Kung, PP; Sinnema, PJ; Richardson, P; Hickey, MJ; Gajiwala, KS; Wang, F; Huang, BW; McClellan, G; Wang, J; Maegley, K; Bergqvist, S; Mehta, PP; Kania, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3557-3562 , 文章类型： Article，,卷期：2011年21-12]
- A series of novel and potent small molecule Hsp90 inhibitors was optimized using X-ray crystal structures. These compounds bind in a deep pocket of the Hsp90 enzyme that is partially comprised by residues Asn51 and Ser52...
|