Volume 22; Issue 15

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Bioorganic & Medicinal Chemistry Letters
Volume 22; Issue 15

Bioorganic & Medicinal Chemistry Letters

Volume 22; Issue 15

1

Synthesis and evaluation of water-soluble resveratrol and piceatannol via BGLation

Hisao Nemoto, Ayato Katagiri, Masaki Kamiya, Tsuyoshi Matsushita, Hatsuhiko Hattori, Kosuke Matsumura, Tomohiro Itou, Tomoyuki Kawamura, Toshiyuki Kita, Hana Nishida, Naokatu Arakaki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 197 KB

english, 2012

2

Design, synthesis and vasodilative activity of tanshinone IIA derivatives

Yue-Feng Bi, Zhen-Ji Wang, Ruo-Fei Guan, Yu-Ting Ye, Yuan-Yuan Chen, Yan-Bing Zhang, Hong-Min Liu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 441 KB

english, 2012

3

Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential

Anette Graven Sams, Krestian Larsen, Gitte Kobberøe Mikkelsen, Morten Hentzer, Claus Tornby Christoffersen, Klaus Gjervig Jensen, Kristen Frederiksen, Benny Bang-Andersen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 717 KB

english, 2012

4

Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives

Ravindra B. Pathak, P.T. Chovatia, H.H. Parekh

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 217 KB

english, 2012

5

Design and synthesis of novel p38α MAP kinase inhibitors: Discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety

Tadamasa Arai, Michihiro Ohno, Hideki Inoue, Shinnosuke Hayashi, Takumi Aoki, Hiroe Hirokawa, Hiroyuki Meguro, Yoko Koga, Keiyu Oshida, Mie Kainoh, Kazuharu Suyama, Hideki Kawai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.00 MB

english, 2012

6

Synthesis and in vitro evaluation of [18F](R)-FEPAQ: A potential PET ligand for VEGFR2

Jaya Prabhakaran, Victoria Arango, Vattoly J. Majo, Norman R. Simpson, Suham A. Kassir, Mark D. Underwood, Hanish Polavarapu, Jeffrey N. Bruce, Peter Canoll, J. John Mann, J.S. Dileep Kumar

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 235 KB

english, 2012

7

Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR

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

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.50 MB

english, 2012

8

Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

Kevin K.-C. Liu, Simon Bailey, Dac M. Dinh, Hieu Lam, Chunze Li, Peter A. Wells, Min-Jean Yin, Aihua Zou

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 828 KB

english, 2012

9

Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor

Jon-Paul Strachan, Jarrett J. Farias, Jenny Zhang, William S. Caldwell, Balwinder S. Bhatti

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 428 KB

english, 2012

10

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

James M. Salovich, Paige N. Vinson, Douglas J. Sheffler, Atin Lamsal, Thomas J. Utley, Anna L. Blobaum, Thomas M. Bridges, Uyen Le, Carrie K. Jones, Michael R. Wood, J. Scott Daniels, P. Jeffrey Conn,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 4.28 MB

english, 2012

11

Synthesis and biological evaluation of novel 2,4,6-triazine derivatives as antimicrobial agents

Sandip N. Gavade, Vijay L. Markad, Kisan M. Kodam, Murlidhar S. Shingare, Dhananjay V. Mane

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 224 KB

english, 2012

12

Synthesis and SAR studies of bicyclic amine series GPR119 agonists

Masao Sakairi, Masakazu Kogami, Masafumi Torii, Hiroyo Kataoka, Hiroki Fujieda, Mitsuhiro Makino, Daisuke Kataoka, Ryuji Okamoto, Toshiyuki Miyazawa, Morio Okabe, Megumi Inoue, Naoki Takahashi, Satoko

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 764 KB

english, 2012

13

Enamino-oxindole HIV protease inhibitors

Michael Eissenstat, Tanya Guerassina, Sergei Gulnik, Elena Afonina, Abelardo M. Silva, Douglas Ludtke, Hiroko Yokoe, Betty Yu, John Erickson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 851 KB

english, 2012

14

Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: Synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies

Hiroshi Nagase, Satomi Imaide, Shigeto Hirayama, Toru Nemoto, Hideaki Fujii

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 682 KB

english, 2012

15

The potential role of anibamine, a natural product CCR5 antagonist, and its analogues as leads toward development of anti-ovarian cancer agents

Yan Zhang, Christopher K. Arnatt, Feng Zhang, Jiannan Wang, Kendra M. Haney, Xianjun Fang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 255 KB

english, 2012

16

Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV

John I. Manchester, Daemian D. Dussault, Jonathan A. Rose, P. Ann Boriack-Sjodin, Maria Uria-Nickelsen, Georgine Ioannidis, Shanta Bist, Paul Fleming, Kenneth G. Hull

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.47 MB

english, 2012

17

Discovery of benzylisothioureas as potent divalent metal transporter 1 (DMT1) inhibitors

Zaihui Zhang, Vishnumurthy Kodumuru, Serguei Sviridov, Shifeng Liu, Mikhail Chafeev, Sultan Chowdhury, Nagasree Chakka, Jianyu Sun, Simon J. Gauthier, Maryanne Mattice, Laszlo G. Ratkay, Rainbow Kwan,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.39 MB

english, 2012

18

Discovery and optimization of novel fatty acid transport protein 1 (FATP1) inhibitors

Tetsuyoshi Matsufuji, Mika Ikeda, Asuka Naito, Masakazu Hirouchi, Hideo Takakusa, Shoichi Kanda, Masanori Izumi, Jun Harada, Tsuyoshi Shinozuka

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.15 MB

english, 2012

19

InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents

Naveen Mulakayala, Bhaskar Kandagatla, Ismail, Rajesh Kumar Rapolu, Pallavi Rao, Chaitanya Mulakayala, Chitta Suresh Kumar, Javed Iqbal, Srinivas Oruganti

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 949 KB

english, 2012

20

Identification of the actinorhodin monomer and its related compound from a deletion mutant of the actVA-ORF4 gene of Streptomyces coelicolor A3(2)

Takaaki Taguchi, Takayuki Ebihara, Atsushi Furukawa, Yumiko Hidaka, Ryuji Ariga, Susumu Okamoto, Koji Ichinose

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 575 KB

english, 2012

21

Guanacastane-type diterpenoids with cytotoxic activity from Coprinus plicatilis

Yuanzhen Liu, Yaoyao Li, Yixin Ou, Shuyan Xiao, Chunhua Lu, Zhonghui Zheng, Yuemao Shen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 356 KB

english, 2012

22

Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation

Dennis S.B. Ongarora, Jiri Gut, Philip J. Rosenthal, Collen M. Masimirembwa, Kelly Chibale

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 540 KB

english, 2012

23

Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives

Finn K. Hansen, Mehdi Khankischpur, Ibrahim Tolaymat, Renata Mesaros, Gerd Dannhardt, Detlef Geffken

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 450 KB

english, 2012

24

Synthesis and in vitro antitumor activity of novel scopoletin derivatives

Wukun Liu, Jie Hua, Jinpei Zhou, Huibin Zhang, Haiyang Zhu, Yanhua Cheng, Ronald Gust

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 304 KB

english, 2012

25

A simple solid phase, peptide-based fluorescent assay for the efficient and universal screening of HRV 3C protease inhibitors

Katrin Schünemann, Stephen Connelly, Renata Kowalczyk, Jonathan Sperry, Ian A. Wilson, John D. Fraser, Margaret A. Brimble

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 584 KB

english, 2012

26

Synthesis and biological evaluation of rebeccamycin analogues modified at the imide moiety

Fabio Animati, Marco Berettoni, Mario Bigioni, Monica Binaschi, Amalia Cipollone, Clelia Irrissuto, Federica Nardelli, Lauso Olivieri

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 528 KB

english, 2012

27

Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2

Aditya Sudheer Vaidya, Bhargava Karumudi, Emma Mendonca, Antonett Madriaga, Hazem Abdelkarim, Richard B. van Breemen, Pavel A. Petukhov

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 749 KB

english, 2012

28

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012

Bruce J. Melancon, Thomas J. Utley, Christian Sevel, Margrith E. Mattmann, Yiu-Yin Cheung, Thomas M. Bridges, Ryan D. Morrison, Douglas J. Sheffler, Colleen M. Niswender, J. Scott Daniels, P. Jeffrey

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 4.06 MB

english, 2012

29

Oxoquinoline acyclonucleoside phosphonate analogues as a new class of specific inhibitors of human immunodeficiency virus type 1

Letícia V. Faro, Jéssica M. de Almeida, Cláudio C. Cirne-Santos, Viveca A. Giongo, Luís R. Castello-Branco, Ingrid de B. Oliveira, Juliana E.F. Barbosa, Anna C. Cunha, Vítor F. Ferreira, Marcos C. de

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 276 KB

english, 2012

30

Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors

Frank Bennett, Hollis S. Kezar III, Vinay Girijavallabhan, Yuhua Huang, Regina Huelgas, Randall Rossman, Neng-Yang Shih, John J. Piwinski, Malcolm MacCoss, Cecil D. Kwong, Jeremy L. Clark, Anita T. Fo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.52 MB

english, 2012

31

Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors

Tim H.M. Jonckers, Marie-Claude Rouan, Geerwin Haché, Wim Schepens, Sabine Hallenberger, Judith Baumeister, Jennifer C. Sasaki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 530 KB

english, 2012

32

γ-Butyrobetaine hydroxylase catalyses a Stevens type rearrangement

Luc Henry, Ivanhoe K.H. Leung, Timothy D.W. Claridge, Christopher J. Schofield

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 490 KB

english, 2012

33

Synthesis of vanadyl–hypocrellin A complex and its photodynamic properties research

Chao Yang, Fei Ma, Jing Tang, Lina Han, Shaohua Wei, Lin Zhou, Jiahong Zhou, Jian Shen, Fang Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 600 KB

english, 2012

34

Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity

Stella Peña, Laura Scarone, Eduardo Manta, Lindsay Stewart, Vanessa Yardley, Simon Croft, Gloria Serra

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 584 KB

english, 2012

35

The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors

Moon H. Kim, Amy Lew Tsuhako, Erick W. Co, Dana T. Aftab, Frauke Bentzien, Jason Chen, Wei Cheng, Stefan Engst, Levina Goon, Rhett R. Klein, Donna T. Le, Morrison Mac, Jason J. Parks, Fawn Qian, Monic

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 999 KB

english, 2012

36

Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine

Soon Goo Lee, Tara D. Alpert, Joseph M. Jez

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 788 KB

english, 2012

37

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Emily A. Peterson, Alessandro A. Boezio, Paul S. Andrews, Christiane M. Boezio, Tammy L. Bush, Alan C. Cheng, Deborah Choquette, James R. Coats, Adria E. Colletti, Katrina W. Copeland, Michelle DuPont

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 814 KB

english, 2012

38

Synthesis and structure–activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists

Carolyn D. Dzierba, Thais M. Sielecki, Argyrios G. Arvanitis, Amy Galka, Tricia L. Johnson, Amy G. Takvorian, Maria Rafalski, Padmaja Kasireddy-Polam, Shikha Vig, Bireshwar Dasgupta, Ge Zhang, Thaddeu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 783 KB

english, 2012

39

Discovery and optimization of novel purines as potent and selective CB2 agonists

Sean P. Hollinshead, Peter C. Astles, Mark G. Chambers, Michael P. Johnson, John Palmer, Michael W. Tidwell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 535 KB

english, 2012

40

Discovery of ITX 4520: A highly potent orally bioavailable hepatitis C virus entry inhibitor

Gopi Kumar Mittapalli, Fang Zhao, Andrew Jackson, Hongfeng Gao, Haekyung Lee, Stephine Chow, Maninder Pal Kaur, Natalie Nguyen, Robert Zamboni, Jeffrey McKelvy, Flossie Wong-Staal, James E. Macdonald

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 6.32 MB

english, 2012

41

Synthesis and antibacterial activity against Clostridium difficile of novel demethylvancomycin derivatives

Si-Ji Zhang, Qing Yang, Liang Xu, Jun Chang, Xun Sun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 251 KB

english, 2012

42

Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening

Hwangseo Park, Soyoung Lee, Sungwoo Hong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 687 KB

english, 2012

43

Discovery and structure–activity relationships of urea derivatives as potent and novel CCR3 antagonists

Aiko Nitta, Yosuke Iura, Hiroki Tomioka, Ippei Sato, Koichiro Morihira, Hirokazu Kubota, Tatsuaki Morokata, Makoto Takeuchi, Mitsuaki Ohta, Shin-ichi Tsukamoto, Takayuki Imaoka, Toshiya Takahashi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.04 MB

english, 2012

44

Activity-based fluorescent probes for monitoring sulfatase activity

Hyun-Joo Park, Hyun-Woo Rhee, Jong-In Hong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 418 KB

english, 2012

45

Antimycobacterial activity: A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines

Ang Chee Wei, Mohamed Ashraf Ali, Yeong Keng Yoon, Rusli Ismail, Tan Soo Choon, Raju Suresh Kumar, Natarajan Arumugam, Abdulrahman I. Almansour, Hasnah Osman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 500 KB

english, 2012

46

Effect of substitution at N″-position of N′-hydroxy-N-amino guanidines on tumor cell growth

Arijit Basu, Barij Nayan Sinha, Philipp Saiko, Thomas Szekeres

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 341 KB

english, 2012

47

Synthesis and evaluation of aplysinopsin analogs as inhibitors of human monoamine oxidase A and B

Kevin Lewellyn, Dobroslawa Bialonska, Narayan D. Chaurasiya, Babu L. Tekwani, Jordan K. Zjawiony

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 410 KB

english, 2012

48

Erratum to “Discovery of XL413, a potent and selective CDC7 inhibitor” [Bioorg. Med. Chem. Lett. 22 (2012) 3727–3731]

Elena S. Koltun, Amy Lew Tsuhako, David S. Brown, Naing Aay, Arlyn Arcalas, Vicky Chan, Hongwang Du, Stefan Engst, Kim Ferguson, Maurizio Franzini, Adam Galan, Charles R. Holst, Ping Huang, Brian Kane

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 114 KB

english, 2012

49

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 31 KB

english, 2012

50

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.30 MB

english, 2012

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