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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共67条记录   3D-QSAR Study on dihydro-1,3,5-triazines and their spiro derivatives as DHFR inhibitors by comparative molecular field analysis (CoMFA) [作者：Ma, X; Xiang, GY; Yap, CW; Chui, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3194-3197 , 文章类型： Article，,卷期：2012年22-9] A 3D-QSAR/CoMFA was performed for a series of triazine and its spiro derivative based DHFR inhibitors displaying IC50 values ranging from 0.002 to 58.8 mu M. Analyses resulted in a reliable computational model with the p... Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent beta isoform selective phosphatidylinositol 3-kinase inhibitors [作者：Sanchez, RM; Erhard, K; Hardwicke, MA; Lin, H; McSurdy-Freed, J; Plant, R; Raha, K; Rominger, CM; Schaber, MD; Spengler, MD; Moore, ML; Yu, HY; Luengo, JI; Tedesco, R; Rivero, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3198-3202 , 文章类型： Article，,卷期：2012年22-9] A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds i... Lead optimization of 4,4-biaryl piperidine amides as gamma-secretase inhibitors [作者：Close, J; Heidebrecht, R; Hendrix, J; Li, CM; Munoz, B; Surdi, L; Kattar, S; Tempest, P; Moses, P; Geng, XL; Hughes, B; Smotrov, N; Moxham, C; Chapnick, J; Kariv, I; Nikov, G; Burke, JE; Deshmukh, S; Jeliazkova-Mecheva, V; Leach, JK; Diaz, D; Xu, L; Yang, ZP; Kwei, G; Moy, L; Shah, S; Tanga, F; Kenefic, C; Savage, D; Shearman, M; Ball, RG; McNevin, MJ; Markarewicz, A; Miller, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3203-3207 , 文章类型： Article，,卷期：2012年22-9] Alzheimer's disease is a major unmet medical need with pathology characterized by extracellular pro-teinaceous plaques comprised primarily of beta-amyloid. gamma-Secretase is a critical enzyme in the cellular pathway res... Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families [作者：Curtin, ML; Frey, RR; Heyman, HR; Soni, NB; Marcotte, PA; Pease, LJ; Glaser, KB; Magoc, TJ; Tapang, P; Albert, DH; Osterling, DJ; Olson, AM; Bouska, JJ; Guan, ZW; Preusser, LC; Polakowski, JS; Stewart, KD; Tse, C; Davidsen, SK; Michaelides, MR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3208-3212 , 文章类型： Article，,卷期：2012年22-9] In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of th... Development of hydrocortisone succinic acid/and 5-fluorouracil/chitosan microcapsules for oral and topical drug deliveries [作者：Lam, PL; Lee, KKH; Wong, RSM; Cheng, GYM; Cheng, SY; Yuen, MCW; Lam, KH; Gambari, R; Kok, SHL; Chui, CH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3213-3218 , 文章类型： Article，,卷期：2012年22-9] Recently, we demonstrated the safety use of calendula oil/chitosan microcapsules as a carrier for both oral and topical deliveries. We also reported the improved biological activity towards skin cells and Staphylococcus ... Anti-AIDS agents 89. Identification of DCX derivatives as anti-HIV and chemosensitizing dual function agents to overcome P-gp-mediated drug resistance for AIDS therapy [作者：Zhou, T; Ohkoshi, E; Shi, Q; Bastow, KF; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3219-3222 , 文章类型： Article，,卷期：2012年22-9] In this study, 19 dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-dihydropyranoxanth-one (DCX) derivatives, previously discovered as novel anti-HIV agents, were evaluated for their potential to reverse multi-dr... Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation [作者：Banerjee, A; Yadav, PS; Bajpai, M; Sangana, RR; Gullapalli, S; Gudi, GS; Gharat, LA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3223-3228 , 文章类型： Article，,卷期：2012年22-9] The synthesis and structure-activity relationship studies of isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors are discussed. The pharmacokinetic profile of 10 and 21 with adequate CNS penetration, required ... 5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors [作者：Arasappan, A; Bennett, F; Girijavallabhan, V; Huang, YH; Huelgas, R; Alvarez, C; Chen, L; Gavalas, S; Kim, SH; Kosinski, A; Pinto, P; Rizvi, R; Rossman, R; Shankar, B; Tong, L; Velazquez, F; Venkatraman, S; Verma, VA; Kozlowski, J; Shih, NY; Piwinski, JJ; MacCoss, M; Kwong, CD; Clark, JL; Fowler, AT; Geng, F; Kezar, HS; Roychowdhury, A; Reynolds, RC; Maddry, JA; Ananthan, S; Secrist, JA; Li, C; Chase, R; Curry, S; Huang, HC; Tong, X; Njoroge, FG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3229-3234 , 文章类型： Article，,卷期：2012年22-9] Based on a previously identified HCV replication (replicase) inhibitor 1, SAR efforts were conducted around the pyrimidine core to improve the potency and pharmacokinetic profile of the inhibitors. A benzothiazole moiety... 4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators [作者：Jimenez, HN; Liu, KG; Hong, SP; Reitman, MS; Uberti, MA; Bacolod, MD; Cajina, M; Nattini, M; Sabio, M; Doller, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3235-3239 , 文章类型： Article，,卷期：2012年22-9] 4-(1-Phenyl-1H-pyrazol-4-yl)quinoline (1) was identified by screening the Lundbeck compound collection, and characterized as having mGlu4 receptor positive allosteric modulator properties. Compound 1 is selective over ot... A conformationally restricted uniconazole analogue as a specific inhibitor of rice ent-kaurene oxidase, CYP701A6 [作者：Todoroki, Y; Naiki, K; Muramatsu, T; Ohnishi, T; Ueno, K; Mizutani, M; Hirai, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3240-3243 , 文章类型： Article，,卷期：2012年22-9] The plant growth retardant uniconazole (UNI), which has been used as an effective inhibitor of ent-kaurene oxidase (CYP701A) involved in gibberellin biosynthesis, also strongly inhibits ABA 8'-hydroxylase (CYP707A), a ke... Analogs of the RSK inhibitor SL0101: Optimization of in vitro biological stability [作者：Hilinski, MK; Mrozowski, RM; Clark, DE; Lannigan, DA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3244-3247 , 文章类型： Article，,卷期：2012年22-9] The Ser/Thr protein kinase, RSK, is important in the etiology of tumor progression including invasion and motility. The natural product kaempferol-3-O-(3",4"-di-O-acetyl-alpha-L-rhamnopyranoside), called SL0101, is a hig... Conformationally restricted novel pyrazole derivatives: Synthesis of 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles as a new class of PDE4 inhibitors [作者：Reddy, TS; Kumar, KS; Meda, CLT; Kandale, A; Rambabu, D; Krishna, GR; Hariprasad, C; Rao, VV; Venkataiah, S; Reddy, CM; Naidu, A; Dubey, PK; Parsa, KVL; Pal, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3248-3255 , 文章类型： Article，,卷期：2012年22-9] A number of novel 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles based on a conformationally restricted pyrazole framework have been designed as potential inhibitors of PDE4. All these compounds were rea... Novel acridinedione derivatives: Design, synthesis, SIRT1 enzyme and tumor cell growth inhibition studies [作者：Alvala, M; Bhatnagar, S; Ravi, A; Jeankumar, VU; Manjashetty, TH; Yogeeswari, P; Sriram, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3256-3260 , 文章类型： Article，,卷期：2012年22-9] A new scaffold N-(9-(ortho/meta/para-(benzyloxy)phenyl)-3,3,6,6-tetramethyl-1,8-dioxo-1,2,3,4,5,6,7,8-octahydroacridin- 10(9H)-yl) isonicotinamide (H1-3) was discovered as a hSIRT1 inhibitor through virtual screening of ... Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor [作者：Chen, SK; Zhao, P; Shao, YX; Li, Z; Zhang, CX; Liu, PQ; He, XX; Luo, HB; Hu, XP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3261-3264 , 文章类型： Article，,卷期：2012年22-9] Phosphodiesterase-4 (PDE4) has been identified to be a promising target for treatment of asthma. Moracin M extracted from Chinese herbal drug 'Sang-Bai-Pi' (Morus alba L.) was studied for the inhibitory affinity towards ... Discovery of 4 '-azido-2 '-deoxy-2 '-C-methyl cytidine and prodrugs thereof: A potent inhibitor of Hepatitis C virus replication [作者：Nilsson, M; Kalayanov, G; Winqvist, A; Pinho, P; Sund, C; Zhou, XX; Wahling, H; Belfrage, AK; Pelcman, M; Agback, T; Benckestock, K; Wikstrom, K; Boothee, M; Lindqvist, A; Rydegard, C; Jonckers, THM; Vandyck, K; Raboisson, P; Lin, TI; Lachau-Durand, S; de Kock, H; Smith, DB; Martin, JA; Klumpp, K; Simmen, K; Vrang, L; Terelius, Y; Samuelsson, B; Rosenquist, A; Johansson, NG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3265-3268 , 文章类型： Article，,卷期：2012年22-9] 4'-Azido-2'-deoxy-2'-methylcytidine (14) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC50 value of 1.2 mu M and showing moderate in vivo bioavailability in rat (F = 14%). ... New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line [作者：Kim, HJ; Cho, HJ; Kim, H; El-Gamal, MI; Oh, CH; Lee, SH; Sim, T; Hah, JM; Yoo, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3269-3273 , 文章类型： Article，,卷期：2012年22-9] A series of new diarylurea and diarylamide derivatives possessing acet(benz)amidophenyl scaffold was synthesized. Their in vitro antiproliferative activity was tested against A375P human melanoma cell line. Compounds 1c,...