Bioorganic and Medicinal Chemistry Letters Table of Contents: 2009, vol. 19, No. 24

Editorial board

IFC
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Graphical contents list

6819-6829
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Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability
David J. Richard, Jeroen C. Verheijen, Kevin Curran, Joshua Kaplan, Lourdes Toral-Barza, Irwin Hollander, Judy Lucas, Ker Yu, Arie Zask
6830-6835

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N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases
Oscar Saavedra, Stephen Claridge, Lijie Zhan, Franck Raeppel, Marie-Claude Granger, Stéphane Raeppel, Michael Mannion, Frédéric Gaudette, Nancy Zhou, Ljubomir Isakovic, Naomy Bernstein, Robert Déziel, Hannah Nguyen, Normand Beaulieu, Carole Beaulieu, Isabelle Dupont, James Wang, A. Robert Macleod, Jeffrey M. Besterman, Arkadii Vaisburg
6836-6839

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Tetrahydroquinoline derivatives as CRTH2 antagonists
Jiwen Liu, Yingcai Wang, Ying Sun, Derek Marshall, Shichang Miao, George Tonn, Penny Anders, Joel Tocker, H. Lucy Tang, Julio Medina
6840-6844

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Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors
Vinod D. Jadhav, Adam S. Duerfeldt, Brian S.J. Blagg
6845-6850

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Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA
Katherine A. Rawls, P. Therese Lang, Jun Takeuchi, Shinichi Imamura, Tyler D. Baguley, Christoph Grundner, Tom Alber, Jonathan A. Ellman
6851-6854

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Synthesis and biological evaluation of salicylic acid and N-acetyl-2-carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: Dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity
Morshed A. Chowdhury, Khaled R.A. Abdellatif, Ying Dong, Dipankar Das, Gang Yu, Carlos A. Velázquez, Mavanur R. Suresh, Edward E. Knaus
6855-6861

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Metal-mediated inhibition is a viable approach for inhibiting cellular methionine aminopeptidase
Sergio C. Chai, Qi-Zhuang Ye
6862-6864

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Synthesis and monoamine transporter affinity of 3α-arylmethoxy-3β-arylnortropanes
Harneet Kaur, Sari Izenwasser, Abha Verma, Dean Wade, Amy Housman, Edwin D. Stevens, David L. Mobley, Mark L. Trudell
6865-6868

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Development of photoaffinity probes for γ-secretase equipped with a nitrobenzenesulfonamide-type cleavable linker
Satoshi Yokoshima, Yuzo Abe, Naoto Watanabe, Yoichi Kita, Toshiyuki Kan, Takeshi Iwatsubo, Taisuke Tomita, Tohru Fukuyama
6869-6871

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Structure–activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: Toward selective Abl inhibitors
Christophe Antczak, Darren R. Veach, Christina N. Ramirez, Maria A. Minchenko, David Shum, Paul A. Calder, Mark G. Frattini, Bayard Clarkson, Hakim Djaballah
6872-6876

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Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
Binhua Lv, Baihua Xu, Yan Feng, Kun Peng, Ge Xu, Jiyan Du, Lili Zhang, Wenbin Zhang, Ting Zhang, Liangcheng Zhu, Haifeng Ding, Zelin Sheng, Ajith Welihinda, Brian Seed, Yuanwei Chen
6877-6881

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Aroylguanidine-based factor Xa inhibitors: The discovery of BMS-344577
Yan Shi, Chi Li, Stephen P. O’Connor, Jing Zhang, Mengxiao Shi, Sharon N. Bisaha, Ying Wang, Doree Sitkoff, Andrew T. Pudzianowski, Christine Huang, Herbert E. Klei, Kevin Kish, Joseph Yanchunas Jr., Eddie C.-K. Liu, Karen S. Hartl, Steve M. Seiler, Thomas E. Steinbacher, William A. Schumacher, Karnail S. Atwal, Philip D. Stein
6882-6889

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Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors
Ariamala Gopalsamy, Greg Ciszewski, Mengxiao Shi, Dan Berger, Yongbo Hu, Frederick Lee, Larry Feldberg, Eileen Frommer, Steven Kim, Karen Collins, Donald Wojciechowicz, Robert Mallon
6890-6892

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Multivalent binding oligomers inhibit HIV Tat–TAR interaction critical for viral replication
Deyun Wang, Jaclyn Iera, Heather Baker, Priscilla Hogan, Roger Ptak, Lu Yang, Tracy Hartman, Robert W. Buckheit Jr., Alexandre Desjardins, Ao Yang, Pascale Legault, Venkat Yedavalli, Kuan-Teh Jeang, Daniel H. Appella
6893-6897

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Synthesis and anticancer activity of sclerophytin-inspired hydroisobenzofurans
T. David Bateman, Aarti L. Joshi, Kwangyul Moon, Elena N. Galitovskaya, Meenakshi Upreti, Timothy C. Chambers, Matthias C. McIntosh
6898-6901

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Identification of novel agonists of the integrin CD11b/CD18
Mohd. Hafeez Faridi, Dony Maiguel, Constantinos J. Barth, Darren Stoub, Ruth Day, Stephan Schürer, Vineet Gupta
6902-6906

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Structural insights into IKKβ inhibition by natural products staurosporine and quercetin
Carolina M. Avila, Nelilma C. Romeiro, Carlos M.R. Sant’Anna, Eliezer J. Barreiro, Carlos A.M. Fraga
6907-6910

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Synthesis, spectroscopic properties and protein labeling of water soluble 3,5-disubstituted boron dipyrromethenes
Özlem Dilek, Susan L. Bane
6911-6913

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Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine
Iva Fernandes, Nuno Vale, Victor de Freitas, Rui Moreira, Nuno Mateus, Paula Gomes
6914-6917

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Design, synthesis and evaluation of novel oxazaphosphorine prodrugs of 9-(2-phosphonomethoxyethyl)adenine (PMEA, adefovir) as potent HBV inhibitors
Peng Lu, Jiangxia Liu, Yuya Wang, Xiaoyan Chen, Yushe Yang, Ruyun Ji
6918-6921

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COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans
Ericsson David Coy, Luis Enrique Cuca, Michael Sefkow
6922-6925

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New small molecule inhibitors of hepatitis C virus
Wanguo Wei, Cuifang Cai, Smitha Kota, Virginia Takahashi, Feng Ni, A. Donny Strosberg, John K. Snyder
6926-6930

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Effect of chirality of small molecule organofluorine inhibitors of amyloid self-assembly on inhibitor potency
Abha Sood, Mohammed Abid, Samson Hailemichael, Michelle Foster, Béla Török, Marianna Török
6931-6934

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1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT6 receptor ligands
Ronald C. Bernotas, Schuyler A. Antane, Steven E. Lenicek, Simon N. Haydar, Albert J. Robichaud, Boyd L. Harrison, Guo Ming Zhang, Deborah Smith, Joseph Coupet, Lee E. Schechter
6935-6938

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Synthesis and biological evaluation of 2-amino-7,7-dimethyl 4-substituted-5-oxo-1-(3,4,5-trimethoxy)-1,4,5,6,7,8-hexahydro-quinoline-3-carbonitrile derivatives as potential cytotoxic agents
Saleh I. Alqasoumi, Areej M. Al-Taweel, Ahmed M. Alafeefy, Mostafa M. Hamed, Eman Noaman, Mostafa M. Ghorab
6939-6942

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Physicochemical property profiles of marketed drugs, clinical candidates and bioactive compounds
Christian Tyrchan, Niklas Blomberg, Ola Engkvist, Thierry Kogej, Sorel Muresan
6943-6947

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Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs
Rita Fürst, István Zupkó, Ágnes Berényi, Gerhard F. Ecker, Uwe Rinner
6948-6951

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N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase
Simeon Bowers, Gary D. Probst, Anh P. Truong, Roy K. Hom, Andrei W. Konradi, Hing L. Sham, Albert W. Garofalo, Karina Wong, Erich Goldbach, Kevin P. Quinn, John-Michael Sauer, William Wallace, Lan Nguyen, Susanna S. Hemphill, Michael P. Bova, Guriqbal S. Basi
6952-6956

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Novel pyrazolopyrimidines as highly potent B-Raf inhibitors
Martin J. Di Grandi, Dan M. Berger, Darrin W. Hopper, Chunchun Zhang, Minu Dutia, Alejandro L. Dunnick, Nancy Torres, Jeremy I. Levin, George Diamantidis, Christoph W. Zapf, Jonathan D. Bloom, YongBo Hu, Dennis Powell, Donald Wojciechowicz, Karen Collins, Eileen Frommer
6957-6961

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Synthesis and evaluation of a thio analogue of duocarmycin SA
Karen S. MacMillan, James P. Lajiness, Carlota Lopez Cara, Romeo Romagnoli, William M. Robertson, Inkyu Hwang, Pier Giovanni Baraldi, Dale L. Boger
6962-6965

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Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase
Peiqing Zhu, Yi Bi, Jinyi Xu, Zan Li, Jun Liu, Luyong Zhang, Wencai Ye, Xiaoming Wu
6966-6969

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Cell-based optimization of novel benzamides as potential antimalarial leads
Tao Wu, Advait Nagle, Tomoyo Sakata, Kerstin Henson, Rachel Borboa, Zhong Chen, Kelli Kuhen, David Plouffe, Elizabeth Winzeler, Francisco Adrian, Tove Tuntland, Jonathan Chang, Susan Simerson, Steven Howard, Jared Ek, John Isbell, Xianming Deng, Nathanael S. Gray, David C. Tully, Arnab K. Chatterjee
6970-6974

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Synthesis of fluorescent C24-ceramide: Evidence for acyl chain length dependent differences in penetration of exogenous NBD-ceramides into human skin
Jakub Novotný, Kateřina Pospěchová, Alexandr Hrabálek, Robert Čáp, Kateřina Vávrová
6975-6977

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A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors
Shijun Zhang, Ajay Yekkirala, Ye Tang, Philip S. Portoghese
6978-6980

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Synthesis, stereochemistry and antimicrobial studies of novel oxime ethers of aza/diazabicycles
Paramasivam Parthiban, Gopalakrishnan Aridoss, Paramasivam Rathika, Venkatachalam Ramkumar, Senthamaraikannan Kabilan
6981-6985

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NSAID-derived γ-secretase modulators. Part III: Membrane anchoring
Stefanie Baumann, Nicole Höttecke, Robert Schubenel, Karlheinz Baumann, Boris Schmidt
6986-6990

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Imidazo[1,2-a]pyrazine diaryl ureas: Inhibitors of the receptor tyrosine kinase EphB4
Scott A. Mitchell, Mihaela Diana Danca, Peter A. Blomgren, James W. Darrow, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Steven L. Gallion, Jin-Ming Xiong, Douglas A. Pippin, Robert W. DeSimone, David R. Brittelli, David C. Eustice, Aaron Bourret, Melissa Hill-Drzewi, Patricia M. Maciejewski, Lisa L. Elkin
6991-6995

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Synthesis of 9-anilinoacridine triazines as new class of hybrid antimalarial agents
Ashok Kumar, Kumkum Srivastava, S. Raja Kumar, S.K. Puri, Prem M.S. Chauhan
6996-6999

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Synthesis and antimycobacterial evaluation of novel 5,6-dimethoxy-1-oxo-2,5-dihydro-1H-2-indenyl-5,4-substituted phenyl methanone analogues
Mohamed Ashraf Ali, Jeyabalan Govinda Samy, Elumalai Manogaran, Velmurugan Sellappan, Mohamed Zaheen Hasan, Mohamed Jawed Ahsan, Suresh Pandian, Mohammad ShaharYar
7000-7002

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Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates
Steven C. Zammit, Alison J. Cox, Renae M. Gow, Yuan Zhang, Richard E. Gilbert, Henry Krum, Darren J. Kelly, Spencer J. Williams
7003-7006

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Design, synthesis and bioactivity of catechin/epicatechin and 2-azetidinone derived chimeric molecules
Basab Roy, Arindam Chakraborty, Sudip K. Ghosh, Amit Basak
7007-7010

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