Volume 21; Issue 4

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Bioorganic & Medicinal Chemistry Letters
Volume 21; Issue 4

Bioorganic & Medicinal Chemistry Letters

Volume 21; Issue 4

1

Pyrrolidinone diterpenoid from Isodon excisus and inhibition of nitric oxide production in lipopolysaccharide-induced macrophage RAW264.7 cells

Seong Su Hong, Seon A Lee, Nahyun Kim, Ji Sang Hwang, Xiang Hua Han, Mi Kyeong Lee, Jae Kyung Jung, Jin Tae Hong, Youngsoo Kim, Dongho Lee, Bang Yeon Hwang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 214 KB

english, 2011

2

Design and synthesis of highly solvatochromic fluorescent 2′-deoxyguanosine and 2′-deoxyadenosine analogs

Katsuhiko Matsumoto, Naoya Takahashi, Azusa Suzuki, Takashi Morii, Yoshio Saito, Isao Saito

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 641 KB

english, 2011

3

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors

Kevin K.C. Liu, Xiaojun Huang, Shubha Bagrodia, Jeffrey H. Chen, Samantha Greasley, Hengmiao Cheng, Shaoxian Sun, Dan Knighton, Caroline Rodgers, Kristina Rafidi, Aihua Zou, Jiezhan Xiao, Shengyong Ya

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.69 MB

english, 2011

4

The Discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors

Alex J. Buckmelter, Li Ren, Ellen R. Laird, Bryson Rast, Greg Miknis, Steve Wenglowsky, Stephen Schlachter, Mike Welch, Eugene Tarlton, Jonas Grina, Joseph Lyssikatos, Barbara J. Brandhuber, Tony Mora

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 886 KB

english, 2011

5

Synthesis and galectin-binding activities of mercaptododecyl glycosides containing a terminal β-galactosyl group

Teiichi Murakami, Kyoko Yoshioka, Yukari Sato, Mutsuo Tanaka, Osamu Niwa, Soichi Yabuki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 374 KB

english, 2011

6

Chemical and biological explorations of the electrophilic reactivity of the bioactive marine natural product halenaquinone with biomimetic nucleophiles

Jiayi Wang, Marie-Lise Bourguet-Kondracki, Arlette Longeon, Joëlle Dubois, Alexis Valentin, Brent R. Copp

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 306 KB

english, 2011

7

Synthesis and biological evaluation of 2-aminoimidazole/carbamate hybrid anti-biofilm and anti-microbial agents

Steven A. Rogers, Erick A. Lindsey, Daniel C. Whitehead, Trey Mullikin, Christian Melander

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 307 KB

english, 2011

8

Non-oxime inhibitors of B-RafV600E kinase

Li Ren, Steve Wenglowsky, Greg Miknis, Bryson Rast, Alex J. Buckmelter, Robert J. Ely, Stephen Schlachter, Ellen R. Laird, Nikole Randolph, Michele Callejo, Matthew Martinson, Sarah Galbraith, Barbara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.66 MB

english, 2011

9

Discovery of new anti-depressants from structurally novel 5-HT3 receptor antagonists: Design, synthesis and pharmacological evaluation of 3-ethoxyquinoxalin-2-carboxamides

Radhakrishnan Mahesh, Thangaraj Devadoss, Dilip Kumar Pandey, Shvetank Bhatt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 281 KB

english, 2011

10

Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands

Guiying Li, Hao Zhou, Yu Jiang, Holger Keim, Sidney W. Topiol, Suresh B. Poda, Yong Ren, Gamini Chandrasena, Darío Doller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 561 KB

english, 2011

11

Pyridylmethylthio derivatives as VEGF inhibitors: Part 2

Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Yoshimasa Sasabuchi, Minoru Yamamoto, Masakazu Ban, Kazuyoshi Okamoto, Kenji Inoue, Takaaki Inaba, Yuriko Takeno, Takashi Tsuboi, Asaka Tonouchi, Hiroy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 647 KB

english, 2011

12

Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): Discovery of EPPTB (RO5212773)

Henri Stalder, Marius C. Hoener, Roger D. Norcross

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 929 KB

english, 2011

13

Furoxan nitric oxide donor coupled chrysin derivatives: Synthesis and vasculoprotection

Xiao-Qing Zou, Sheng-Ming Peng, Chang-Ping Hu, Li-Feng Tan, Han-Wu Deng, Yuan-Jian Li

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 354 KB

english, 2011

14

Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors

Eunhyun Choi, Chulho Lee, Jung Eun Park, Jeong Jea Seo, Misun Cho, Jong Soon Kang, Hwan Mook Kim, Song-Kyu Park, Kiho Lee, Gyoonhee Han

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 330 KB

english, 2011

15

Synthesis and antitubercular evaluation of novel substituted aryl and thiophenyl tethered dihydro-6H-quinolin-5-ones

Srinivas Kantevari, Santhosh Reddy Patpi, Balasubramanian Sridhar, Perumal Yogeeswari, Dharmarajan Sriram

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 375 KB

english, 2011

16

Design and regioselective synthesis of a new generation of targeted therapeutics. Part 3: Folate conjugates of aminopterin hydrazide for the treatment of inflammation

Iontcho R. Vlahov, Fei You, Hari Krishna R. Santhapuram, Yu Wang, Jeremy F. Vaughn, Spencer J. Hahn, Paul J. Kleindl, Mingjin Fan, Christopher P. Leamon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 546 KB

english, 2011

17

Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene

Jonathan Y. Bass, Justin A. Caravella, Lihong Chen, Katrina L. Creech, David N. Deaton, Kevin P. Madauss, Harry B. Marr, Robert B. McFadyen, Aaron B. Miller, Wendy Y. Mills, Frank Navas III, Derek J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.88 MB

english, 2011

18

6″-Azido-6″-deoxy-UDP-N-acetylglucosamine as a glycosyltransferase substrate

Alain Mayer, Tracey M. Gloster, Wayne K. Chou, David J. Vocadlo, Martin E. Tanner

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 322 KB

english, 2011

19

Triaryl (Z)-olefins suitable for radiolabeling with iodine-124 or fluorine-18 radionuclides for positron emission tomography imaging of estrogen positive breast tumors

Khaled R.A. Abdellatif, Carlos A. Velázquez, Zhangjian Huang, Morshed A. Chowdhury, Edward E. Knaus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 257 KB

english, 2011

20

Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy

Meizhong Jin, Andrew Kleinberg, Andy Cooke, Prafulla C. Gokhale, Kenneth Foreman, Hanqing Dong, Kam W. Siu, Mark A. Bittner, Kristen M. Mulvihill, Yan Yao, Darla Landfair, Matthew O’Connor, Gilda Mak,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 981 KB

english, 2011

21

Synthesis and pharmacological evaluation of the individual stereoisomers of 3-[methyl(1,2,3,4-tetrahydro-2-naphthalenyl)amino]-1-indanone, a potent mast cell stabilising agent

Adam J. Byrne, James W. Barlow, John J. Walsh

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 433 KB

english, 2011

22

Improved synthesis of 5-hydroxymethyl-2′-deoxycytidine phosphoramidite using a 2′-deoxyuridine to 2′-deoxycytidine conversion without temporary protecting groups

Anders S. Hansen, Armin Thalhammer, Afaf H. El-Sagheer, Tom Brown, Christopher J. Schofield

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 436 KB

english, 2011

23

Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase

Elizabeth Fullam, Areej Abuhammad, David L. Wilson, Matthew C. Anderton, Steve G. Davies, Angela J. Russell, Edith Sim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.10 MB

english, 2011

24

Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation

Carmela Napolitano, Alessandro Natoni, Corrado Santocanale, Lasse Evensen, James B. Lorens, Paul V. Murphy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 431 KB

english, 2011

25

Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor

Cheng-Shi Jiang, Rong Zhou, Jing-Xu Gong, Li-Li Chen, Tibor Kurtán, Xu Shen, Yue-Wei Guo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 385 KB

english, 2011

26

Potent radiosensitizing agents: 5-Methylselenyl- and 5-phenylselenyl-methyl-2′-deoxyuridine

Ambadas B. Rode, Byeong Mo Kim, Seon Hwa Park, In Seok Hong, Sung Hee Hong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 687 KB

english, 2011

27

HIV-1 protease inhibition potential of functionalized polyoxometalates

Andreas Flütsch, Thilo Schroeder, Markus G. Grütter, Greta R. Patzke

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 577 KB

english, 2011

28

Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors

Peter Ray, Jane Wright, Julia Adam, Sylviane Boucharens, Darcey Black, Angus R. Brown, Ola Epemolu, Dan Fletcher, Margaret Huggett, Phil Jones, Steven Laats, Amanda Lyons, Jos de Man, Richard Morphy,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.14 MB

english, 2011

29

Spirodiketopiperazine-based CCR5 antagonist: Discovery of an antiretroviral drug candidate

Rena Nishizawa, Toshihiko Nishiyama, Katsuya Hisaichi, Chiaki Minamoto, Naoki Matsunaga, Yoshikazu Takaoka, Hisao Nakai, Stephen Jenkinson, Wieslaw M. Kazmierski, Hideaki Tada, Kenji Sagawa, Shiro Shi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 433 KB

english, 2011

30

Design and synthesis of potent Gram-negative specific LpxC inhibitors

U. Faruk Mansoor, Dilrukshi Vitharana, Panduranga Adulla Reddy, Dayna L. Daubaras, Paul McNicholas, Peter Orth, Todd Black, M. Arshad Siddiqui

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 3.91 MB

english, 2011

31

Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging

Yunpeng Ye, Lei Zhu, Ying Ma, Gang Niu, Xiaoyuan Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 635 KB

english, 2011

32

Synthesis and biophysical characterization of R-6′-Me-α-l-LNA modified oligonucleotides

Punit P. Seth, Jinghua Yu, Charles R. Allerson, Andres Berdeja, Eric E. Swayze

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 519 KB

english, 2011

33

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity

Hawa Diallo, Davina C. Angell, Heather A. Barnett, Keith Biggadike, Diane M. Coe, Tony W.J. Cooper, Andy Craven, James R. Gray, David House, Torquil I. Jack, Steve P. Keeling, Simon J.F. Macdonald, Ia

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.54 MB

english, 2011

34

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties

Hans G.F. Richter, G.M. Benson, K.H. Bleicher, D. Blum, E. Chaput, N. Clemann, S. Feng, C. Gardes, U. Grether, P. Hartman, B. Kuhn, R.E. Martin, J.-M. Plancher, M.G. Rudolph, F. Schuler, S. Taylor

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 708 KB

english, 2011

35

Synthesis, structure–activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

Zhao Wang, Xuan-Hong Shi, Jia Wang, Tian Zhou, You-Zhi Xu, Ting-Ting Huang, Yan-Fang Li, Ying-Lan Zhao, Li Yang, Sheng-Yong Yang, Luo-Ting Yu, Yu-Quan Wei

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 465 KB

english, 2011

36

Investigation on a host–guest inclusion system by β-cyclodextrin derivative and its analytical application

Lizhen Huang, Jiang He, Ruihua Lu, Xia Ge, Jingjing Guo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 448 KB

english, 2011

37

A unique and rapid approach toward the efficient development of novel protein tyrosine phosphatase (PTP) inhibitors based on ‘clicked’ pseudo-glycopeptides

Jin-Wei Yang, Xiao-Peng He, Cui Li, Li-Xin Gao, Li Sheng, Juan Xie, Xiao-Xin Shi, Yun Tang, Jia Li, Guo-Rong Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 505 KB

english, 2011

38

Identification of small molecular inhibitors for Ero1p by structure-based virtual screening

Yanyan Chu, Xianjun Chen, Yi Yang, Yun Tang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 684 KB

english, 2011

39

Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas

Hao Peng, Yongju Liang, Le Chen, Liwu Fu, Haiqin Wang, Hongwu He

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 200 KB

english, 2011

40

Discovery of dual binding site acetylcholinesterase inhibitors identified by pharmacophore modeling and sequential virtual screening techniques

Shikhar Gupta, Adyary Fallarero, Päivi Järvinen, Daniela Karlsson, Mark S. Johnson, Pia M. Vuorela, C. Gopi Mohan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 960 KB

english, 2011

41

Synthesis and evaluation of trehalose-based compounds as anti-invasive agents

Yong-Li Jiang, Long-Qian Tang, Satoshi Miyanaga, Yasuhiro Igarashi, Ikuo Saiki, Zhao-Peng Liu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 252 KB

english, 2011

42

Corrigendum to “Natural products-based insecticidal agents 4. Semisynthesis and insecticidal activity of novel esters of 2-chloropodophyllotoxin against Mythimna separata Walker in vivo” [Bioorg. Med. Chem. Lett. 19 (2009) 5415]

Hui Xu, Xiao Xiao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 118 KB

english, 2011

43

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 32 KB

english, 2011

44

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1.79 MB

english, 2011

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