- Modulation of PPAR receptor subtype selectivity of the ligands: Aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety
[作者:Pingali, H; Jain, M; Shah, S; Patil, P; Makadia, P; Zaware, P; Sairam, KVVM; Jamili, J; Goel, A; Patel, M; Patel, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6471-6475 , 文章类型: Article,,卷期:2008年18-24]
- Oxazole containing glycine and oximinobutyric acid derivatives were synthesized as PPAR alpha agonists by incorporating polymethylene spacer as a replacement of commonly used phenylene group that connects the acidic head...
- Oxinobactin, a siderophore analogue to enterobactin involving 8-hydroxyquinoline subunits: Synthesis and iron binding ability
[作者:d'Hardemare, AD; Alnaga, N; Serratrice, G; Pierre, JL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6476-6478 , 文章类型: Article,,卷期:2008年18-24]
- Oxinobactin, a siderophore analogue to enterobactin but possessing 8-hydroxyquinoline instead of catechol complexing subunits, has been synthesized starting from L-serine and 8-hydroxyquinoline. Comparative iron binding ...
- Calmodulin inhibitory activity of the malbrancheamides and various analogs
[作者:Miller, KA; Figueroa, M; Valente, MWN; Greshock, TJ; Mata, R; Williams, RM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6479-6481 , 文章类型: Article,,卷期:2008年18-24]
- The preparation and biological activity of various structural analogs of the malbrancheamides are disclosed. The impact of indole chlorination, C-12a relative stereochemistry, and bicyclo[2.2.2]diazaoctane core oxidation...
- alpha-Mercaptoketone based histone deacetylase inhibitors
[作者:Wash, PL; Hoffman, TZ; Wiley, BM; Bonnefous, C; Smith, ND; Sertic, MS; Lawrence, CM; Symons, KT; Nguyen, PM; Lustig, KD; Guo, X; Annable, T; Noble, SA; Hager, JH; Hassig, CA; Malecha, JW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6482-6485 , 文章类型: Article,,卷期:2008年18-24]
- In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel alpha-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number o...
- Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors
[作者:Jones, CD; Andrew, DM; Barker, AJ; Blades, K; Byth, KF; Raymond, M; Finlay, V; Geh, C; Green, CP; Johannsen, M; Walker, M; Weir, HM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6486-6489 , 文章类型: Article,,卷期:2008年18-24]
- The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative...
- Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors
[作者:Yi, W; Cao, R; Wen, H; Yan, Q; Zhou, B; Wan, Y; Ma, L; Song, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6490-6493 , 文章类型: Article,,卷期:2008年18-24]
- A series of helicid analogues were synthesized and evaluated as tyrosinase inhibitors. The results demonstrated that some compounds had more potent inhibitory activities than arbutin (IC50 7.3 mM). In particular, compoun...
- Five-coordinated oxovanadium(IV) complexes derived from amino acids and ciprofloxacin: Synthesis, spectral, antimicrobial, and DNA interaction approach
[作者:Patel, MN; Patel, SH; Chhasatia, MR; Parmar, PA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6494-6500 , 文章类型: Article,,卷期:2008年18-24]
- Five-coordinated oxovanadium(IV) complexes with ciprofloxacin and various uninegative bidentate amino acids have been prepared. The structure of complexes has been investigated using spectral, physicochemical, mass spect...
- The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901
[作者:Barrett, SD; Bridges, AJ; Dudley, DT; Saltiel, AR; Fergus, JH; Flamme, CM; Delaney, AM; Kaufman, M; LePage, S; Leopold, WR; Przybranowski, SA; Sebolt-Leopold, J; Van Becelaere, K; Doherty, AM; Kennedy, RM; Marston, D; Howard, WA; Smith, Y; Warmus, JS; Tecle, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6501-6504 , 文章类型: Article,,卷期:2008年18-24]
- A novel series of benzhydroxamate esters derived from their precursor anthranilic acids have been prepared and have been identified as potent MEK inhibitors. 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-diflu...
- Novel anthraquinone derivatives: Synthesis via click chemistry approach and their induction of apoptosis in BGC gastric cancer cells via reactive oxygen species(ROS)-dependent mitochondrial pathway
[作者:Wang, SR; Wang, QL; Wang, Y; Liu, L; Weng, XC; Li, G; Zhang, XL; Zhou, X,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6505-6508 , 文章类型: Article,,卷期:2008年18-24]
- Three water soluble anthraquinone derivatives were designed and synthesized employing click chemistry to prepare novel and potent antitumor drugs. An MTT assay indicated that all compounds had significant inhibitory acti...
- cis-Nitromethylene neonicotinoids as new nicotinic family: Synthesis, structural diversity, and insecticidal evaluation of hexahydroimidazo[1,2-alpha]pyridine
[作者:Shao, XS; Zhang, WW; Peng, YQ; Li, Z; Tian, ZZ; Qian, XH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6513-6516 , 文章类型: Article,,卷期:2008年18-24]
- A series of neonicotinoids analogues of hexahydroimidazo[1,2-alpha]pyridine were modified at 5-, 6-, and 7-positions, and their insecticidal activities were evaluated. Introducing a methyl or ethyl at 7-position increase...
- Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum
[作者:Martyn, DC; Ramirez, AP; Berattie, MJ; Cortese, JF; Patel, V; Rush, MA; Woerpel, KA; Clardy, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6521-6524 , 文章类型: Article,,卷期:2008年18-24]
- Artemisinin-derived compounds play an integral role in current malaria chemotherapy. Given the virtual certainty of emerging resistance, we have investigated spiro-1,2-dioxolanes as an alternative scaffold. The endoperox...
- Synthesis of 3,6-bicyclolides: A novel class of macrolide antibiotics
[作者:Gai, YH; Tang, DT; Xu, GY; Chen, ZG; Polemeropoulos, A; Wang, Z; Or, YS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6315-6318 , 文章类型: Article,,卷期:2008年18-24]
- The synthesis of 3,6-bicyclolides from erythromycin A oxime is described. This novel class of bridged bicyclic macrolides demonstrates potent in vitro and in vivo activities against a broad spectrum of bacteria including...
- Leucettamol A: A new inhibitor of Ubc13-Uev1A interaction isolated from a marine sponge, Leucetta aff. microrhaphis
[作者:Tsukamoto, S; Takeuchi, T; Rotinsulu, H; Mangindaan, REP; van Soest, RWM; Ukai, K; Kobayashi, H; Namikoshi, M; Ohta, T; Yokosawa, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6319-6320 , 文章类型: Article,,卷期:2008年18-24]
- A compound that inhibits the formation of a complex composed of the ubiquitin E2 enzyme Ubc13 and Uev1A was isolated from the marine sponge Leucetta aff. microrhaphis. The compound was identified as leucettamol A (1) by ...
- New cyclic tetrapeptides from Nonomuraea sp TA-0426 that inhibit glycine transporter type 1 (GlyT1)
[作者:Terui, Y; Yi-wen, C; Jun-ying, L; Ando, T; Fukunaga, T; Aoki, T; Toda, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6321-6323 , 文章类型: Article,,卷期:2008年18-24]
- In the course of our search for natural antipsychotic agents, we isolated five new cyclic tetrapeptides from the fermentation broth of Nonomuraea sp. TA-0426. These compounds turned out to be analogues of WSS2220, which ...
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