- 2 '-Fluorosugar analogues of the highly potent anti-varicella-zoster virus bicyclic nucleoside analogue (BCNA) Cf 1743
[作者：McGuigan, C; Derudas, M; Quintiliani, M; Andrei, G; Snoeck, R; Henson, G; Balzarini, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6264-6267 , 文章类型： Article，,卷期：2009年19-22]
- We report the preparation of 2 '-alpha-F, 2 '-beta-F and 2 ',2 '-difluoro analogues of the leading anti-varicella zoster virus (VZV) pentylphenyl BCNA Cf 1743. VZV thymidine kinase showed the highest phosphorylating capa...
- Synthesis of 4-mercapto-L-lysine derivatives: Potential building blocks for sequential native chemical ligation
[作者：Pasunooti, KK; Yang, RL; Vedachalam, S; Gorityala, BK; Liu, CF; Liu, XW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6268-6271 , 文章类型： Article，,卷期：2009年19-22]
- A general and diastereoselective synthesis of (2S, 4S)-4-mercapto-L-lysine derivative was described. The key features of this synthesis include Zn-mediated diastereoselective Reformatsky reaction and selective reduction ...
- Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives
[作者：Candea, ALP; Ferreira, MD; Pais, KC; Cardoso, LND; Kaiser, CR; Henriques, MDGMD; Lourenco, MCS; Bezerra, FAF; de Souza, MVN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6272-6274 , 文章类型： Article，,卷期：2009年19-22]
- A series of twenty-one 7-chloro-4-quinolinylhydrazones (3a-u) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv. The compounds 3f, 3i and 3o were non...
- Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051
[作者：Enache, LA; Zhang, J; Sullins, DW; Kennedy, I; Onua, E; Zembower, DE; Muellner, FW; Singh, J; Kiselyov, AS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6275-6279 , 文章类型： Article，,卷期：2009年19-22]
- The same two major CYP mediated metabolites of DG-051 were produced in the presence of rat, dog, monkey and human liver microsomes. Their respective structures were hypothesized based on mass spectrometry data correlated...
- Ionic liquid mediated and promoted eco-friendly preparation of thiazolidinone and pyrimidine nucleoside-thiazolidinone hybrids and their antiparasitic activities
[作者：Zhang, XY; Li, XY; Li, DF; Qu, GR; Wang, JJ; Loiseau, PM; Fan, XS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6280-6283 , 文章类型： Article，,卷期：2009年19-22]
- Without any catalyst, 2,3-disubstituted-1,3-thiazolidin-4-one derivatives were synthesized efficiently via the three-component reaction of aldehyde, amine and mercaptoacetic acid in [bmim][PF6]. The whole procedure is si...
- Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group
[作者：Su, H; Yu, LQ; Nebbioso, A; Carafa, V; Chen, YD; Altucci, L; You, QD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6284-6288 , 文章类型： Article，,卷期：2009年19-22]
- Ongoing effort to gather further knowledge about the structural requirements on histone deacetylase inhibitors led to the synthesis of novel N-hydroxybenzamide-based HDAC inhibitors 1a-o, introducing branched hydrophobic...
- Antitumor agents 269. Non-aromatic ring-A neotanshinlactone analog, TNO, as a new class of potent antitumor agents
[作者：Dong, YZ; Shi, QA; Nakagawa-Goto, K; Wu, PC; Bastow, KF; Morris-Natschke, SL; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6289-6292 , 文章类型： Article，,卷期：2009年19-22]
- Tetrahydroneotanshinlactone (TNT) and tetrahydronaphthalene-1-ol (TNO) derivatives were designed, synthesized, and evaluated for cytotoxic activity. The TNO derivatives were found to be a promising novel class of in vitr...
- Synthesis and biological evaluation of p38 alpha kinase-targeting dialkynylimidazoles
[作者：Li, J; Kaoud, TS; Laroche, C; Dalby, KN; Kerwin, SM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6293-6297 , 文章类型： Article，,卷期：2009年19-22]
- Based on the mild, thermal rearrangement of 1,2-dialkynylimidazoles to reactive carbene or diradical intermediates, a series of 1,2-dialkynylimidazoles were designed as potential irreversible p38 MAP kinase a-isoform (p3...
- Synthetic peptides containing a conserved sequence motif of the Id protein family modulate vascular smooth muscle cell phenotype
[作者：Pellegrino, S; Ferri, N; Colombo, N; Cremona, E; Corsini, A; Fanelli, R; Gelmi, ML; Cabrele, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6298-6302 , 文章类型： Article，,卷期：2009年19-22]
- Modulation of smooth muscle cells to a proliferating and migrating phenotype with downregulated alpha-actin expression is observed upon vascular lesion formation. The Id proteins (inhibitors of cell differentiation) play...
- Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin
[作者：Jung, M; Park, N; Moon, HI; Lee, Y; Chung, WY; Park, KK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6303-6306 , 文章类型： Article，,卷期：2009年19-22]
- Novel amide derivatives of C-12 non-acetal deoxoartemisinin were synthesized. Some of the derivatives had potent in vitro anticancer activity against major human cancer cell lines. The deoxoartemisinin amide trimer had p...
- Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors
[作者：Boezio, AA; Berry, L; Albrecht, BK; Bauer, D; Bellon, SF; Bode, C; Chen, A; Choquette, D; Dussault, I; Hirai, S; Kaplan-Lefko, P; Larrow, JF; Lin, MHJ; Lohman, J; Potashman, MH; Rex, K; Santostefano, M; Shah, K; Shimanovich, R; Springer, SK; Teffera, Y; Yang, YJ; Zhang, YH; Harmange, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6307-6312 , 文章类型： Article，,卷期：2009年19-22]
- Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. We previously showed that O-linked triazolopyridazines can be...
- Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis
[作者：Horita, Y; Takii, T; Chiba, T; Kuroishi, R; Maeda, Y; Kurono, Y; Inagaki, E; Nishimura, K; Yamamoto, Y; Abe, C; Mori, M; Onozaki, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6313-6316 , 文章类型： Article，,卷期：2009年19-22]
- A series of sugar derivatives (1-13) were synthesized and evaluated for antibacterial activity against Mycobacterium tuberculosis (MTB), especially multi-drug resistant (MDR) MTB, and the structure-activity relationships...
- Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog
[作者：Peng, LF; Stanton, BZ; Maloof, N; Wang, X; Schreiber, SL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6319-6325 , 文章类型： Article，,卷期：2009年19-22]
- We report the synthesis and biological activity of a library of aminoalcohol-derived macrocycles from which robotnikinin (17), a binder to and inhibitor of Sonic Hedgehog, was derived. Using an asymmetric alkylation to s...
- Synthesis and antioxidant properties of dendritic polyphenols
[作者：Lee, CY; Sharma, A; Cheong, JE; Nelson, JL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6326-6330 , 文章类型： Article，,卷期：2009年19-22]
- Three dendritic polyphenols (generation 1) were synthesized: a syringaldehyde-based dendrimer (1), a vanillin-based dendrimer (2), and an iodinated vanillin-based dendrimer (3). They all showed strong antioxidant activit...
- Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase
[作者：Popovici-Muller, J; Shipps, GW; Rosner, KE; Deng, YQ; Wang, T; Curran, PJ; Brown, MA; Siddiqui, MA; Cooper, AB; Duca, J; Cable, M; Girijavallabhan, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6331-6336 , 文章类型： Article，,卷期：2009年19-22]
- The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low na...
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