Volume 24; Issue 21

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Bioorganic & Medicinal Chemistry Letters
Volume 24; Issue 21

Bioorganic & Medicinal Chemistry Letters

Volume 24; Issue 21

1

Two new spirooxindole alkaloids from rhizosphere strain Streptomyces sp. xzqh-9

Guo, Kai, Fang, Tingting, Wang, Jingyi, Wu, An-an, Wang, Yuezhou, Jiang, Jie, Wu, Xinrui, Song, Siyang, Su, Wenjing, Xu, Qingyan, Deng, Xianming

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 789 KB

english, 2014

2

New antibacterial xanthone from the marine sponge-derived Micrococcus sp. EG45

Eltamany, Enas E., Abdelmohsen, Usama Ramadan, Ibrahim, Amany K., Hassanean, Hashim A., Hentschel, Ute, Ahmed, Safwat A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 361 KB

english, 2014

3

Discovery of a 1,2-bis(3-indolyl)ethane that selectively inhibits the pyruvate kinase of methicillin-resistant Staphylococcus aureus over human isoforms

Zoraghi, Roya, Campbell, Sara, Kim, Catrina, Dullaghan, Edie M., Blair, Lachlan M., Gillard, Rachel M., Reiner, Neil E., Sperry, Jonathan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 545 KB

english, 2014

4

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway

LaPorte, Matthew G., da Paz Lima, Dimas José, Zhang, Feng, Sen, Malabika, Grandis, Jennifer R., Camarco, Daniel, Hua, Yun, Johnston, Paul A., Lazo, John S., Resnick, Lynn O., Wipf, Peter, Huryn, Donna

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.43 MB

english, 2014

5

Two new antioxidant actinosporin analogues from the calcium alginate beads culture of sponge-associated Actinokineospora sp. strain EG49

Grkovic, Tanja, Abdelmohsen, Usama Ramadan, Othman, Eman Maher, Stopper, Helga, Edrada-Ebel, RuAngelie, Hentschel, Ute, Quinn, Ronald J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 389 KB

english, 2014

6

Discovery of a nanomolar inhibitor of lung adenocarcinoma in vitro

Shelton, Jadd R., Balzarini, Jan, Peterson, Matt A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 732 KB

english, 2014

7

Synthesis, characterization, molecular docking and anti-tubercular activity of Plumbagin–Isoniazid Analog and its β-cyclodextrin conjugate

Dandawate, Prasad, Vemuri, Kiranmayi, Venkateswara Swamy, K., Khan, Ejazuddin M., Sritharan, Manjula, Padhye, Subhash

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.37 MB

english, 2014

8

Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide

Altimari, Jarrad M., Niranjan, Birunthi, Risbridger, Gail P., Schweiker, Stephanie S., Lohning, Anna E., Henderson, Luke C.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.43 MB

english, 2014

9

Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents

Draffan, Alistair G., Frey, Barbara, Fraser, Benjamin H., Pool, Brett, Gannon, Carlie, Tyndall, Edward M., Cianci, Julia, Harding, Michael, Lilly, Michael, Hufton, Richard, Halim, Rosliana, Jahangiri,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 815 KB

english, 2014

10

Design, synthesis, and structure–activity relationship of novel opioid κ receptor selective agonists: α-Iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton

Watanabe, Yoshikazu, Kitazawa, Shota, Fujii, Hideaki, Nemoto, Toru, Hirayama, Shigeto, Iwai, Takashi, Gouda, Hiroaki, Hirono, Shuichi, Nagasea, Hiroshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 853 KB

english, 2014

11

Inhibition of the ANT(2″)-Ia resistance enzyme and rescue of aminoglycoside antibiotic activity by synthetic α-hydroxytropolones

Hirsch, Danielle R., Cox, Georgina, D’Erasmo, Michael P., Shakya, Tushar, Meck, Christine, Mohd, Noushad, Wright, Gerard D., Murelli, Ryan P.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.22 MB

english, 2014

12

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I

Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castro, Jordi, Eastwood, Paul R., Eichhorn, Peter, Esteve, Cristina, Gómez, Elena, González, Jacob, Mir, Marta,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.24 MB

english, 2014

13

Oxo- and thiooxo-imidazo[1,5-c]pyrimidine molecule library: Beyond their interest in inhibition of Brucella suis histidinol dehydrogenase, a powerful protection tool in the synthesis of histidine analogues

Turtaut, François, Lopez, Marie, Ouahrani-Bettache, Safia, Köhler, Stephan, Winum, Jean-Yves

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 498 KB

english, 2014

14

Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists

Kim, Kyoung Soon, Zhang, Liping, Williams, David, Perez, Heidi L., Stang, Erik, Borzilleri, Robert M., Posy, Shana, Lei, Ming, Chaudhry, Charu, Emanuel, Stuart, Talbott, Randy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.88 MB

english, 2014

15

Synthesis and structure–activity relationship of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents

Yang, Jun, Zhou, Shanshan, Ji, Liyan, Zhang, Chao, Yu, Siwang, Li, Zhongjun, Meng, Xiangbao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.11 MB

english, 2014

16

Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1

Desrat, Sandy, Pujals, Anaïs, Colas, Claire, Dardenne, Jérémy, Gény, Charlotte, Favre, Loëtitia, Dumontet, Vincent, Iorga, Bogdan I., Litaudon, Marc, Raphaël, Martine, Wiels, Joëlle, Roussi, Fanny

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 653 KB

english, 2014

17

Bioavailable pyrrolo-benzo-1,4-diazines as Nav1.7 sodium channel blockers for the treatment of pain

Yang, Shu-Wei, Ho, Ginny D., Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A., Herr, R. Jason, Zhou, Xiaoping, Brida

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.70 MB

english, 2014

18

Discovery of potent and selective GIRK1/2 modulators via ‘molecular switches’ within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas

Wen, Wandong, Wu, Wenjun, Weaver, C. David, Lindsley, Craig W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 928 KB

english, 2014

19

Vanillin-derived antiproliferative compounds influence Plk1 activity

Carrasco-Gomez, Roberto, Keppner-Witter, Sarah, Hieke, Martina, Lange, Lisa, Schneider, Gisbert, Schubert-Zsilavecz, Manfred, Proschak, Ewgenij, Spänkuch, Birgit

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.79 MB

english, 2014

20

Glutathione-S-transferase selective release of metformin from its sulfonamide prodrug

Rautio, Jarkko, Vernerová, Monika, Aufderhaar, Imke, Huttunen, Kristiina M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 259 KB

english, 2014

21

Structure–activity relationships of non-opioid [des-Arg7]-dynorphin A analogues for bradykinin receptors

Lee, Yeon Sun, Rankin, David, Hall, Sara M., Ramos-Colon, Cyf, Ortiz, Jose Juan, Kupp, Robert, Porreca, Frank, Lai, Josephine, Hruby, Victor J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 235 KB

english, 2014

22

Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

Kang, Seung-Tae, Kim, Eun-Young, Archary, Raghavendra, Jung, Heejung, Park, Chi Hoon, Yun, Chang-Soo, Hwang, Jong Yeon, Choi, Sang Un, Chae, Chonghak, Lee, Chong Ock, Kim, Hyoung Rae, Ha, Jae Du, Ryu,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.31 MB

english, 2014

23

Deuteration and fluorination of 1,3-bis(2-phenylethyl)pyrimidine-2,4,6(1H,3H,5H)-trione to improve its pharmacokinetic properties

Xia, Guoyao, Benmohamed, Radhia, Morimoto, Richard I., Kirsch, Donald R., Silverman, Richard B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 970 KB

english, 2014

24

In vitro apoptotic effect of cassaine-type diterpene amides from Erythrophleum fordii on PC-3 prostate cancer cells

Hung, Tran Manh, Cuong, To Dao, Kim, Jeong Ah, Lee, Jeong Hyung, Woo, Mi Hee, Min, Byung Sun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 760 KB

english, 2014

25

Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors

Bruel, Amélie, Bénéteau, Romain, Chabanne, Mylène, Lozach, Olivier, Le Guevel, Rémy, Ravache, Myriam, Bénédetti, Hélène, Meijer, Laurent, Logé, Cédric, Robert, Jean-Michel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.22 MB

english, 2014

26

Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)–1H-imidazolium salts

Xu, Xiao-Liang, Wang, Jia, Yu, Chun-Lei, Chen, Wen, Li, Ying-Chao, Li, Yan, Zhang, Hong-Bin, Yang, Xiao-Dong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 670 KB

english, 2014

27

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: Lead optimization

Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Calbet, Marta, Eastwood, Paul R., Eichhorn, Peter, Esteve, Cristina, Ferrer, Manel, Gómez, Elena, González, Jacob, Mir, Marta, Moreno, Imma, Petit,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.07 MB

english, 2014

28

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists

Andrés, Miriam, Buil, Maria Antonia, Calbet, Marta, Casado, Oscar, Castro, Jordi, Eastwood, Paul R., Eichhorn, Peter, Ferrer, Manel, Forns, Pilar, Moreno, Imma, Petit, Silvia, Roberts, Richard S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.26 MB

english, 2014

29

Rational design, synthesis and anti-proliferative evaluation of novel benzosuberone tethered with hydrazide–hydrazones

Yadagiri, Bandi, Holagunda, Uma Devi, Bantu, Rajashaker, Nagarapu, Lingaiah, Guguloth, Vijayacharan, Polepally, Sowjanya, Jain, Nishanth

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 618 KB

english, 2014

30

Synthesis of new 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles: A search for novel nitric oxide donor anti-inflammatory agents

Abdellatif, Khaled R.A., Moawad, Abeer, Knaus, Edward E.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.34 MB

english, 2014

31

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: The role of a hydrogen-bond acceptor in long receptor residence times

Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castro, Jordi, Eastwood, Paul R., Esteve, Cristina, Ferrer, Manel, Forns, Pilar, Gómez, Elena, González, Jacob,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.22 MB

english, 2014

32

Design, synthesis and exploring the quantitative structure–activity relationship of some antioxidant flavonoid analogues

Das, Sreeparna, Mitra, Indrani, Batuta, Shaikh, Niharul Alam, Md., Roy, Kunal, Begum, Naznin Ara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 639 KB

english, 2014

33

An eco-friendly and water mediated product selective synthesis of 2-aminopyrimidines and their in vitro anti-bacterial evaluation

Nagarajan, Sangaraiah, Shanmugavelan, Poovan, Sathishkumar, Murugan, Selvi, Ramasamy, Ponnuswamy, Alagusundaram, Harikrishnan, Hariharan, Shanmugaiah, Vellasamy, Murugavel, Saminathan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 4.67 MB

english, 2014

34

The discovery of isoxazoline oxime ethers as a new class of ectoparasiticides for the control of Haematobia irritans (horn fly) in cattle

Curtis, Michael P., Chubb, Nathan, Ellsworth, Edmund, Goodwin, Richard, Holzmer, Sue, Koch, Jason, McTier, Tom, Menon, Sanjay, Mills, Kent, Pullins, Aleah, Stuk, Tim, Zinser, Erich

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.19 MB

english, 2014

35

Discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis biofilms using a scaffold hopping strategy

Abouelhassan, Yasmeen, Garrison, Aaron T., Burch, Gena M., Wong, Wilson, Norwood, Verrill M., Huigens, Robert W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 572 KB

english, 2014

36

Study the interactions between human serum albumin and two antifungal drugs: Fluconazole and its analogue DTP

Zhang, Shao-Lin, Yao, Huankai, Wang, Chenyin, Tam, Kin Y.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 824 KB

english, 2014

37

Antimycobacterial activity generated by the amide coupling of (−)-fenchone derived aminoalcohol with cinnamic acids and analogues

Slavchev, Ivaylo, Dobrikov, Georgi M., Valcheva, Violeta, Ugrinova, Iva, Pasheva, Evdokia, Dimitrov, Vladimir

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 320 KB

english, 2014

38

Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors for the treatment of metabolic disorders

Yoon, David S., Wu, Shung C., Seethala, Ramakrishna, Golla, Rajasree, Nayeem, Akbar, Everlof, John G., Gordon, David A., Hamann, Lawrence G., Robl, Jeffrey A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 863 KB

english, 2014

39

Discovery of substituted 4-aminoquinazolines as selective Toll-like receptor 4 ligands

Nour, Afshin, Hayashi, Tomoko, Chan, Michael, Yao, Shiyin, Tawatao, Rommel I., Crain, Brian, Tsigelny, Igor F., Kouznetsova, Valentina L., Ahmadiiveli, Alast, Messer, Karen, Pu, Minya, Corr, Maripat,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.27 MB

english, 2014

40

Ejection of structural zinc leads to inhibition of γ-butyrobetaine hydroxylase

Rydzik, Anna M., Brem, Jürgen, Struwe, Weston B., Kochan, Grazyna T., Benesch, Justin L.P., Schofield, Christopher J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.44 MB

english, 2014

41

Scaffold hopping towards potent and selective JAK3 inhibitors: Discovery of novel C-5 substituted pyrrolopyrazines

de Vicente, Javier, Lemoine, Remy, Bartlett, Mark, Hermann, Johannes C., Hekmat-Nejad, Mohammad, Henningsen, Robert, Jin, Sue, Kuglstatter, Andreas, Li, Hongju, Lovey, Allen J., Menke, John, Niu, Ling

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.15 MB

english, 2014

42

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 30 KB

english, 2014

43

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.18 MB

english, 2014

44

An update on therapeutic opportunities offered by cancer glycolytic metabolism

Granchi, Carlotta, Fancelli, Daniele, Minutolo, Filippo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.06 MB

english, 2014

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