Volume 22; Issue 21

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Bioorganic & Medicinal Chemistry Letters
Volume 22; Issue 21

Bioorganic & Medicinal Chemistry Letters

Volume 22; Issue 21

1

Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates

Sund, Christian, Belda, Oscar, Borkakoti, Neera, Lindberg, Jimmy, Derbyshire, Dean, Vrang, Lotta, Hamelink, Elizabeth, Åhgren, Cathrine, Woestenenk, Esmeralda, Wikström, Kristina, Eneroth, Anders, Lin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 865 KB

english, 2012

2

4-Substituted-2-phenylquinazolines as inhibitors of BCRP

Juvale, Kapil, Wiese, Michael

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 426 KB

english, 2012

3

Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors

Rambabu, D., Mulakayala, Naveen, Ismail,, Ravi Kumar, K., Pavan Kumar, G., Mulakayala, Chaitanya, Kumar, Chitta Suresh, Kalle, Arunasree M., Basaveswara Rao, M.V., Oruganti, Srinivas, Pal, Manojit

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.27 MB

english, 2012

4

Novel histone deacetylase 8 ligands without a zinc chelating group: Exploring an ‘upside-down’ binding pose

Vaidya, Aditya Sudheer, Neelarapu, Raghupathi, Madriaga, Antonett, Bai, He, Mendonca, Emma, Abdelkarim, Hazem, van Breemen, Richard B., Blond, Sylvie Y., Petukhov, Pavel A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 672 KB

english, 2012

5

Novel 3-substituted-1-aryl-5-phenyl-6-anilinopyrazolo[3,4-d]pyrimidin-4-ones: Docking, synthesis and pharmacological evaluation as a potential anti-inflammatory agents

Yewale, Sandeep B., Ganorkar, Saurabh B., Baheti, Kamalkishor G., Shelke, Rupesh U.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 234 KB

english, 2012

6

Anti-HIV-1 activity of resveratrol derivatives and synergistic inhibition of HIV-1 by the combination of resveratrol and decitabine

Clouser, Christine L., Chauhan, Jay, Bess, Matthew A., Oploo, Jessica L. van, Zhou, Ding, Dimick-Gray, Sarah, Mansky, Louis M., Patterson, Steven E.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 727 KB

english, 2012

7

Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties

Chang, Dong-Jo, Lee, Sujin, Jang, Jaebong, Kim, Soon-Ok, Kim, Wan-Joo, Suh, Young-Ger

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.04 MB

english, 2012

8

Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor

Maloney, Patrick R., Khan, Pasha, Hedrick, Michael, Gosalia, Palak, Milewski, Monika, Li, Linda, Roth, Gregory P., Sergienko, Eduard, Suyama, Eigo, Sugarman, Eliot, Nguyen, Kevin, Mehta, Alka, Vasile,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.30 MB

english, 2012

9

Discovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance

Giordanetto, Fabrizio, Wållberg, Andreas, Ghosal, Saswati, Iliefski, Tommy, Cassel, Johan, Yuan, Zhong-Qing, von Wachenfeldt, Henrik, Andersen, Søren M., Inghardt, Tord, Tunek, Anders, Nylander, Sven

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 605 KB

english, 2012

10

Synthesis and evaluation of naphthoic acid derivatives as fluorescent probes to screen advanced glycation end-products breakers

Séro, Luc, Calard, François, Sanguinet, Lionel, Levillain, Eric, Richomme, Pascal, Séraphin, Denis, Derbré, Séverine

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 977 KB

english, 2012

11

Substituted pyrazolones require N2 hydrogen bond donating ability to protect against cytotoxicity from protein aggregation of mutant superoxide dismutase 1

Trippier, Paul C., Benmohamed, Radhia, Kirsch, Donald R., Silverman, Richard B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 643 KB

english, 2012

12

Formylated polyamines as peptidomimetics

Javor, Sacha, Janowsky, Aaron, Johnson, Robert, Wolfrum, Katherine, Tadayoni-Rebek, Mitra, Rebek, Julius

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 316 KB

english, 2012

13

Identification of a glutathione peroxidase inhibitor that reverses resistance to anticancer drugs in human B-cell lymphoma cell lines

Schulz, Riad, Emmrich, Thomas, Lemmerhirt, Heidi, Leffler, Ulrike, Sydow, Kristin, Hirt, Carsten, Kiefer, Thomas, Link, Andreas, Bednarski, Patrick J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 495 KB

english, 2012

14

Downregulation of mdr1 and abcg2 genes is a mechanism of inhibition of efflux pumps mediated by polymeric amphiphiles

Cuestas, María L., Castillo, Amalia I., Sosnik, Alejandro, Mathet, Verónica L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 204 KB

english, 2012

15

Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors

Lam, Betty, Zhang, Zhiyuan, Stafford, Jeffery A., Skene, Robert J., Shi, Lihong, Gwaltney, Stephen L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 764 KB

english, 2012

16

How hydrogen bonds impact P-glycoprotein transport and permeability

Desai, Prashant V., Raub, Thomas J., Blanco, Maria-Jesus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 826 KB

english, 2012

17

Modifications around the hydroxamic acid chelating group of fosmidomycin, an inhibitor of the metalloenzyme 1-deoxyxylulose 5-phosphate reductoisomerase (DXR)

Zinglé, Catherine, Kuntz, Lionel, Tritsch, Denis, Grosdemange-Billiard, Catherine, Rohmer, Michel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 512 KB

english, 2012

18

Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy

Tamura, Yuusuke, Omori, Naoki, Kouyama, Naoki, Nishiura, Yuji, Hayashi, Kyouhei, Watanabe, Kana, Tanaka, Yukari, Chiba, Takeshi, Yukioka, Hideo, Sato, Hiroki, Okuno, Takayuki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 611 KB

english, 2012

19

3,3′-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding

Weiser, Patrick T., Williams, Anna B., Chang, Ching-Yi, McDonnell, Donald P., Hanson, Robert N.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 228 KB

english, 2012

20

Design, synthesis, spectral and biological evaluation of novel 1-allyl substituted 2,6-diphenylpiperidin-4-ones and its derivatives of oximes/oxime ethers

Narayanan, Kuppusamy, Shanmugam, Mani, Jothivel, Sarangan, Kabilan, Senthamaraikannan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 578 KB

english, 2012

21

Design, synthesis, and structure–activity-relationship of phenyl imidazoles as potent Smoothened antagonists

Cheng, Dai, Han, Dong, Gao, Wenqi, Jing, Qihui, Jiang, Jiqing, Wan, Yongqin, Englund, Nathan P., Tuntland, Tove, Wu, Xu, Pan, Shifeng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.16 MB

english, 2012

22

Design, synthesis and biological activities of sorafenib derivatives as antitumor agents

Yao, Jianwen, He, Zuopeng, Chen, Jing, Sun, Wei, Fang, Hao, Xu, Wenfang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 3.16 MB

english, 2012

23

Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity

Surivet, Jean-Philippe, Lange, Roland, Hubschwerlen, Christian, Keck, Wolfgang, Specklin, Jean-Luc, Ritz, Daniel, Bur, Daniel, Locher, Hans, Seiler, Peter, Strasser, Daniel Stefan, Prade, Lars, Kohl,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.79 MB

english, 2012

24

Synthesis, anti-inflammatory and antimicrobial evaluation of novel 1-acetyl-3,5-diaryl-4,5-dihydro (1H) pyrazole derivatives bearing urea, thiourea and sulfonamide moieties

Keche, Ashish P., Hatnapure, Girish D., Tale, Rajesh H., Rodge, Atish H., Kamble, Vandana M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 244 KB

english, 2012

25

The discovery of CCR3/H1 dual antagonists with reduced hERG risk

Bahl, Ash, Barton, Patrick, Bowers, Keith, Brough, Steven, Evans, Richard, Luckhurst, Christopher A., Mochel, Tobias, Perry, Matthew W.D., Rigby, Aaron, Riley, Robert J., Sanganee, Hitesh, Sisson, Ada

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 498 KB

english, 2012

26

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors

Scott, James S., Gill, Adrian L., Godfrey, Linda, Groombridge, Sam D., Rees, Amanda, Revill, John, Schofield, Paul, Sörme, Pernilla, Stocker, Andrew, Swales, John G., Whittamore, Paul R.O.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 964 KB

english, 2012

27

Chemotherapy of leishmaniasis. Part XI: Synthesis and bioevaluation of novel isoxazole containing heteroretinoid and its amide derivatives

Suryawanshi, S.N., Tiwari, Avinash, Chandra, Naveen, Ramesh,, Gupta, Suman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 846 KB

english, 2012

28

Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-κB activation and PPAR transcriptional activity

Quang, Tran Hong, Ngan, Nguyen Thi Thanh, Minh, Chau Van, Kiem, Phan Van, Yen, Pham Hai, Tai, Bui Huu, Nhiem, Nguyen Xuan, Thao, Nguyen Phuong, Anh, Hoang Le Tuan, Luyen, Bui Thi Thuy, Yang, Seo Young

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 806 KB

english, 2012

29

A hierarchical method for molecular docking using cloud computing

Kang, Ling, Guo, Quan, Wang, Xicheng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 334 KB

english, 2012

30

[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: Introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents

Deskus, Jeffrey A., Dischino, Douglas D., Mattson, Ronald J., Ditta, Jonathan L., Parker, Michael F., Denhart, Derek J., Zuev, Dmitry, Huang, Hong, Hartz, Richard A., Ahuja, Vijay T., Wong, Henry, Mat

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.08 MB

english, 2012

31

Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation

Giordanetto, Fabrizio, Wållberg, Andreas, Cassel, Johan, Ghosal, Saswati, Kossenjans, Michael, Yuan, Zhong-Qing, Wang, Xiaoping, Liang, Lifeng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 741 KB

english, 2012

32

Corrigendum to “Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives” [Bioorg. Med. Chem. Lett. 22 (2012) 5791–5794]

Serra, Silvia, Chicca, Andrea, Delogu, Giovanna, Vázquez-Rodríguez, Saleta, Santana, Lourdes, Uriarte, Eugenio, Casu, Laura, Gertsch, Jürg

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 139 KB

english, 2012

33

Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents

Li, Qing-Shan, Lv, Xian-Hai, Zhang, Yan-Bin, Dong, Jing-Jun, Zhou, Wen-Ping, Yang, Yang, Zhu, Hai-Liang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 744 KB

english, 2012

34

Corrigendum to “Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR” [Bioorg. Med. Chem. Lett. 22 (2012) 5098–5103]

Le, Phuong T., Cheng, Hengmiao, Ninkovic, Sacha, Plewe, Michael, Huang, Xiaojun, Wang, Hai, Bagrodia, Shubha, Sun, Shaoxian, Knighton, Daniel R., LaFleur Rogers, Caroline M., Pannifer, Andrew, Greasle

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 256 KB

english, 2012

35

Effect of substituents at phenyl group of 7,7′-dioxo-9,9′-epoxylignane on antifungal activity

Nishiwaki, Hisashi, Ouchi, Maya, Matsugi, Junko, Akiyama, Koichi, Sugahara, Takuya, Kishida, Taro, Yamauchi, Satoshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 354 KB

english, 2012

36

Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases

Hoque, Md. Ashraful, Arai, Toru, Nishino, Norikazu, Kim, Hyun-Jung, Ito, Akihiro, Yoshida, Minoru

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 417 KB

english, 2012

37

Evaluation of structure-derived pharmacophore of soluble epoxide hydrolase inhibitors by virtual screening

Moser, Daniel, Achenbach, Janosch, Klingler, Franca-Maria, Estel la, Buscató, Hahn, Steffen, Proschak, Ewgenij

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 724 KB

english, 2012

38

Novel sulfanylphthalimide analogues as highly potent inhibitors of monoamine oxidase B

Van der Walt, Mietha M., Terre’Blanche, Gisella, Petzer, Anél, Petzer, Jacobus P.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 292 KB

english, 2012

39

Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation

Yang, Yanhui, Voak, Andrew, Wilkinson, Shane R., Hu, Longqin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 978 KB

english, 2012

40

Design, synthesis and in vitro activities on anti-platelet aggregation of 4-methoxybenzene-1,3-isophthalamides

Liu, Xiu Jie, Shi, Xin Xin, Zhong, Yong Liang, Liu, Ning, Liu, Kai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 3.30 MB

english, 2012

41

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: Possible confounding effects on in vivo and in vitro studies

McElhinny, Charles J., Lewin, Anita H., Mascarella, S. Wayne, Runyon, Scott, Brieaddy, Lawrence, Carroll, F. Ivy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 252 KB

english, 2012

42

Corrigendum to “A highly sensitive fluorescent viscosity sensor” [Bioorg. Med. Chem. Lett. 22 (2012) 5780–5783]

Yusop, Rahimi M., Unciti-Broceta, Asier, Bradley, Mark

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 158 KB

english, 2012

43

Novel cyanocombretastatins as potent tubulin polymerisation inhibitors

Jalily, Pouria H., Hadfield, John A., Hirst, Nicholas, Rossington, Steven B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 741 KB

english, 2012

44

Synthesis and in vitro antitumour screening of 2-(β-d-xylofuranosyl)thiazole-4-carboxamide and two novel tiazofurin analogues with substituted tetrahydrofurodioxol moiety as a sugar mimic

Popsavin, Mirjana, Spaić, Saša, Svirčev, Miloš, Kojić, Vesna, Bogdanović, Gordana, Popsavin, Velimir

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 431 KB

english, 2012

45

Chemotherapy of leishmaniasis. Part IX: Synthesis and bioevaluation of aryl substituted ketene dithioacetals as antileishmanial agents

Kumar, Santosh, Tiwari, Avinash, Suryawanshi, S.N., Mittal, Monika, Vishwakarma, Preeti, Gupta, Suman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 256 KB

english, 2012

46

Acremomannolipin A, the potential calcium signal modulator with a characteristic glycolipid structure from the filamentous fungus Acremonium strictum

Sugiura, Reiko, Kita, Ayako, Tsutsui, Nozomi, Muraoka, Osamu, Hagihara, Kanako, Umeda, Nanae, Kunoh, Tatsuki, Takada, Hirofumi, Hirose, Dai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 614 KB

english, 2012

47

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 3.14 MB

english, 2012

48

Synthesis and in vitro and in vivo anticancer activity of novel 3-methyl-5H-isoxazolo[5′,4′:5,6]pyrido[2,3-b]indoles

Rajanarendar, E., Govardhan Reddy, K., Ramakrishna, S., Nagi Reddy, M., Shireesha, B., Durgaiah, G., Reddy, Y.N.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 225 KB

english, 2012

49

First total synthesis of prasinic acid and its anticancer activity

Chakor, Narayan, Patil, Ganesh, Writer, Diana, Periyasamy, Giridharan, Sharma, Rajiv, Roychowdhury, Abhijit, Mishra, Prabhu Dutt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 312 KB

english, 2012

50

Identification of pyrimidine derivatives as hSMG-1 inhibitors

Gopalsamy, Ariamala, Bennett, Eric M., Shi, Mengxiao, Zhang, Wei-Guo, Bard, Joel, Yu, Ker

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.91 MB

english, 2012

51

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 31 KB

english, 2012

52

Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092

Bahl, Ash, Barton, Patrick, Bowers, Keith, Caffrey, Moya V., Denton, Rebecca, Gilmour, Peter, Hawley, Shaun, Linannen, Tero, Luckhurst, Christopher A., Mochel, Tobias, Perry, Matthew W.D., Riley, Robe

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 901 KB

english, 2012

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