Volume 22; Issue 16

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Bioorganic & Medicinal Chemistry Letters
Volume 22; Issue 16

Bioorganic & Medicinal Chemistry Letters

Volume 22; Issue 16

1

Optimization of acetonitrile co-solvent and copper stoichiometry for pseudo-ligandless click chemistry with nucleic acids

Eduardo Paredes, Subha R. Das

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 260 KB

english, 2012

2

Pyrimidinopyrimidine inhibitors of ketohexokinase: Exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket

Bruce E. Maryanoff, John C. O’Neill, David F. McComsey, Stephen C. Yabut, Diane K. Luci, Alan C. Gibbs, Margery A. Connelly

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 926 KB

english, 2012

3

C3-Heteroaroyl cannabinoids as photolabeling ligands for the CB2 cannabinoid receptor

Darryl D. Dixon, Marcus A. Tius, Ganesh A. Thakur, Han Zhou, Anna L. Bowman, Vidyanand G. Shukla, Yan Peng, Alexandros Makriyannis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 636 KB

english, 2012

4

Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1

Sandra Gemma, Simone Giovani, Margherita Brindisi, Pierangela Tripaldi, Simone Brogi, Luisa Savini, Isabella Fiorini, Ettore Novellino, Stefania Butini, Giuseppe Campiani, Maria Penzo, Michael J. Blac

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 510 KB

english, 2012

5

Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s

Nalin L. Subasinghe, Ehab Khalil, Jeremy M. Travins, Farah Ali, Shelley K. Ballentine, Heather R. Hufnagel, Wenxi Pan, Kristi Leonard, Roger F. Bone, Richard M. Soll, Carl S. Crysler, Nisha Ninan, Jen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.12 MB

english, 2012

6

Antiviral activity and synthesis of quaternized promazine derivatives against HSV-1

Akasha K. Purohit, Matthew D. Balish, Jacob J. Leichty, Ashley Roe, Lori M. Ward, Miguel O. Mitchell, Shao-chung Hsia

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 645 KB

english, 2012

7

Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases

Hwan Geun Choi, Jianming Zhang, Ellen Weisberg, James D. Griffin, Taebo Sim, Nathanael S. Gray

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.81 MB

english, 2012

8

Design, synthesis and antibacterial activities of a series of new 2-oxaisocephems

Jianbo Wu, Xueying Wu, Fan Lei, Huajie Yuan, Li Hai, Yong Wu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.32 MB

english, 2012

9

Synthesis and evaluation of a novel 68Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging

Hee-Jung Kim, Dong-Yeon Kim, Jeong-Hoon Park, Seung-Dae Yang, Min-Goo Hur, Jung-Joon Min, Kook-Hyun Yu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 613 KB

english, 2012

10

Design, synthesis and biological evaluation of novel acrylamide analogues as inhibitors of BCR–ABL kinase

Shuxin Li, Zhenglin Yao, Yanjin Zhao, Wei Chen, Huijia Wang, Xianzhao Kuang, Wenhu Zhan, Shan Yao, Shanyou Yu, Wenxiang Hu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 789 KB

english, 2012

11

Chemoenzymatic deacylation of ramoplanin

Raffaella Gandolfi, Flavia Marinelli, Enzio Ragg, Diego Romano, Francesco Molinari

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 410 KB

english, 2012

12

SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors

Kathryn Bell, Mihiro Sunose, Katie Ellard, Andrew Cansfield, Jess Taylor, Warren Miller, Nigel Ramsden, Giovanna Bergamini, Gitte Neubauer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1004 KB

english, 2012

13

Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1

Zhongsheng Zhang, Kayode K. Ojo, Steven M. Johnson, Eric T. Larson, Penqing He, Jennifer A. Geiger, Alejandro Castellanos-Gonzalez, A. Clinton White Jr., Marilyn Parsons, Ethan A. Merritt, Dustin J. M

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1013 KB

english, 2012

14

Non-canonical regioisomerizations and a ‘Diels–Alderase’ are likely essential in the biosynthesis of Spiculoic acid A

Atahualpa Pinto, Christopher N. Boddy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 559 KB

english, 2012

15

Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α–p300 interaction by a small molecule

Hyuk Sung Kwon, Da-Rae Kim, Eun Gyeong Yang, Yong Keun Park, Hee-Chul Ahn, Sun-Joon Min, Dae-Ro Ahn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 434 KB

english, 2012

16

Eco-friendly synthesis and biological evaluation of substituted pyrano[2,3-c]pyrazoles

Santhosh Reddy Mandha, Sravanthi Siliveri, Manjula Alla, Vittal Rao Bommena, Madhava Reddy Bommineni, Sridhar Balasubramanian

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 496 KB

english, 2012

17

Selective non-lipid modulator of LPA5 activity in human platelets

Detlef H. Kozian, Andreas Evers, Peter Florian, Peter Wonerow, Sabrina Joho, Marc Nazare

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1015 KB

english, 2012

18

The SAR analysis of TRPV1 agonists with the α-methylated B-region

Yongsung Cho, Myeong Seop Kim, Ho Shin Kim, Jihyae Ann, Jiyoun Lee, Larry V. Pearce, Vladimir A. Pavlyukovets, Matthew A. Morgan, Peter M. Blumberg, Jeewoo Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 902 KB

english, 2012

19

Optimisation of imidazole compounds as selective TAAR1 agonists: Discovery of RO5073012

Guido Galley, Henri Stalder, Annick Goergler, Marius C. Hoener, Roger D. Norcross

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.42 MB

english, 2012

20

Triterpenoid saponins from Xanthoceras sorbifolia Bunge and their inhibitory activity on human cancer cell lines

Lili Yu, Xiaobing Wang, Xingchuan Wei, Miaomiao Wang, Lixia Chen, Shijie Cao, Ning Kang, Feng Qiu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 388 KB

english, 2012

21

Corrigendum to “Novel dendrimeric lipopeptides with antifungal activity” [Bioorg. Med. Chem. Lett. 22 (2012) 1388–1393]

Jolanta Janiszewska, Marta Sowińska, Aleksandra Rajnisz, Jolanta Solecka, Izabela Łacka, Sławomir Milewski, Zofia Urbańczyk-Lipkowska

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 119 KB

english, 2012

22

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

John Liddle, Paul Bamborough, Michael D. Barker, Sebastien Campos, Chun-Wa Chung, Rick P.C. Cousins, Paul Faulder, Michelle L. Heathcote, Heather Hobbs, Duncan S. Holmes, Chris Ioannou, Cesar Ramirez-

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.04 MB

english, 2012

23

Supramolecular energy transfer from photoexcited chlorosomal zinc porphyrin self-aggregates to a chlorin or bacteriochlorin monomer as models of main light-harvesting antenna systems in green photosynthetic bacteria

Yumiko Kataoka, Yutaka Shibata, Hitoshi Tamiaki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 555 KB

english, 2012

24

Novel synthetic route to the C-nucleoside, 2-deoxy benzamide riboside

Rebecca R. Midtkandal, Philip Redpath, Samuel A.J. Trammell, Simon J.F. Macdonald, Charles Brenner, Marie E. Migaud

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 268 KB

english, 2012

25

Structural simplification of bioactive natural products with multicomponent synthesis. 4. 4H-Pyrano-[2,3-b]naphthoquinones with anticancer activity

Igor V. Magedov, Artem S. Kireev, Aaron R. Jenkins, Nikolai M. Evdokimov, Dustin T. Lima, Paul Tongwa, Jeff Altig, Wim F. A. Steelant, Severine Van slambrouck, Mikhail Yu. Antipin, Alexander Kornienko

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 684 KB

english, 2012

26

N-Heterocyclic dicarboxylic acids: Broad-spectrum inhibitors of metallo-β-lactamases with co-antibacterial effect against antibiotic-resistant bacteria

Lei Feng, Ke-Wu Yang, Li-Sheng Zhou, Jian-Min Xiao, Xia Yang, Le Zhai, Yi-Lin Zhang, Michael W. Crowder

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 466 KB

english, 2012

27

3-Bromo-3-deazaneplanocin and 3-bromo-3-deazaaristeromycin: Synthesis and antiviral activity

Chong Liu, Qi Chen, Stewart W. Schneller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 303 KB

english, 2012

28

Distinct biological effects of golgicide a derivatives on larval and adult mosquitoes

Daniel J. Mack, Jun Isoe, Roger L. Miesfeld, Jon T. Njardarson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 587 KB

english, 2012

29

Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants

Zhao Dang, Keduo Qian, Phong Ho, Lei Zhu, Kuo-Hsiung Lee, Li Huang, Chin-Ho Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.15 MB

english, 2012

30

A substituted 3,4-dihydropyrimidinone derivative (compound D22) prevents inflammation mediated neurotoxicity; role in microglial activation in BV-2 cells

Oh Wook Kwon, Eunjung Moon, Murugulla A. Chari, Tae Woo Kim, Ae-jung Kim, Pyeongjae Lee, Kwang-Hyun Ahn, Sun Yeou Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 671 KB

english, 2012

31

Discovery of 1-[4-(N-benzylamino)phenyl]-3-phenylurea derivatives as non-peptidic selective SUMO-sentrin specific protease (SENP)1 inhibitors

Masaharu Uno, Yosuke Koma, Hyun Seung Ban, Hiroyuki Nakamura

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 751 KB

english, 2012

32

Investigation of 7-benzylidenenaltrexone derivatives as resistance reverser for chloroquine-resistant Plasmodium chabaudi

Yoshinori Miyata, Hideaki Fujii, Yuka Uenohara, Seiki Kobayashi, Tsutomu Takeuchi, Hiroshi Nagase

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 501 KB

english, 2012

33

The optimization of pyridazinone series of glucan synthase inhibitors

Rongze Kuang, Heping Wu, Pauline C. Ting, Robert G. Aslanian, Jianhua Cao, David W. Kim, Joe F. Lee, John Schwerdt, Gang Zhou, R. Jason Herr, Andrew J. Zych, Jinhai Yang, Sang Q. Lam, David M. Jenkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 3.40 MB

english, 2012

34

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR

Sonia Martínez González, Ana Isabel Hernández, Carmen Varela, Milagros Lorenzo, Francisco Ramos-Lima, Elena Cendón, David Cebrián, Enara Aguirre, Elena Gomez-Casero, M.I. Albarrán, Patricia Alfonso, B

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 968 KB

english, 2012

35

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 31 KB

english, 2012

36

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.07 MB

english, 2012

37

(+)-Pinoresinol is a putative hypoglycemic agent in defatted sesame (Sesamum indicum) seeds though inhibiting α-glucosidase

Arin Wikul, Thanakorn Damsud, Keita Kataoka, Preecha Phuwapraisirisan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 284 KB

english, 2012

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