Volume 23; Issue 12

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Bioorganic & Medicinal Chemistry Letters
Volume 23; Issue 12

Bioorganic & Medicinal Chemistry Letters

Volume 23; Issue 12

1

Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)

Nie, Zhe, Feher, Victoria, Natala, Srinivasa, McBride, Christopher, Kiryanov, Andre, Jones, Benjamin, Lam, Betty, Liu, Yan, Kaldor, Stephen, Stafford, Jeffrey, Hikami, Kouki, Uchiyama, Noriko, Kawamot

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 888 KB

english, 2013

2

Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity

Aytemir, Mutlu Dilsiz, Özçelik, Berrin, Karakaya, Gülşah

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 280 KB

english, 2013

3

Chemical constituents from Nelumbo nucifera leaves and their anti-obesity effects

Ahn, Jong Hoon, Kim, Eun Sil, Lee, Chul, Kim, Soonok, Cho, Soo-Hyun, Hwang, Bang Yeon, Lee, Mi Kyeong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 727 KB

english, 2013

4

Synthesis of new conjugated coumarin–benzimidazole hybrids and their anticancer activity

Paul, Kamaldeep, Bindal, Shweta, Luxami, Vijay

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 845 KB

english, 2013

5

Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole–benzimidazole derivatives as potent Aurora A/B kinase inhibitors

Zheng, Youguang, Zheng, Ming, Ling, Xin, Liu, Yi, Xue, Yunsheng, An, Lin, Gu, Ning, Jin, Min

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 3.10 MB

english, 2013

6

Structural elucidation of novel degradation product of brotizolam

Sugimoto, Yoshinori, Kugimiya, Aya, Yoshimura, Yoshifumi, Naoki, Hideo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 851 KB

english, 2013

7

Synthesis of novel strobilurin–pyrimidine derivatives and their antiproliferative activity against human cancer cell lines

Chai, Baoshan, Wang, Shuyang, Yu, Wenquan, Li, Huichao, Song, Chuanjun, Xu, Ying, Liu, Changling, Chang, Junbiao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 838 KB

english, 2013

8

Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists

Hossain, Nafizal, Ivanova, Svetlana, Bergare, Jonas, Mensonides-Harsema, Marguérite, Cooper, Martin E.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 465 KB

english, 2013

9

Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties

Gong, Leyi, Han, Xiaochun, Silva, Tania, Tan, Yun-Chou, Goyal, Bindu, Tivitmahaisoon, Parch, Trejo, Alejandra, Palmer, Wylie, Hogg, Heather, Jahagir, Alam, Alam, Muzaffar, Wagner, Paul, Stein, Karin,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.74 MB

english, 2013

10

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists

Zhang, Jian (Ken), Li, An-Rong, Yu, Ming, Wang, Yingcai, Zhu, Jiang, Kayser, Frank, Medina, Julio C., Siegler, Karen, Conn, Marion, Shan, Bei, Grillo, Mark P., Eksterowicz, John, Coward, Peter, Liu, J

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.15 MB

english, 2013

11

Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: Development of chemical probe ML315

Coombs, Thomas C., Tanega, Cordelle, Shen, Min, Wang, Jenna L., Auld, Douglas S., Gerritz, Samuel W., Schoenen, Frank J., Thomas, Craig J., Aubé, Jeffrey

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 6.18 MB

english, 2013

12

Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: Synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif

Krueger, A. Chris, Randolph, John T., DeGoey, David A., Donner, Pamela L., Flentge, Charles A., Hutchinson, Douglas K., Liu, Dachun, Motter, Christopher E., Rockway, Todd W., Wagner, Rolf, Beno, David

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 706 KB

english, 2013

13

Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening

Wang, Liyan, Yang, Chunmei, Lu, Weiqiang, Liu, Li, Gao, Rui, Liao, Sha, Zhao, Zhenjiang, Zhu, Lili, Xu, Yufang, Li, Honglin, Huang, Jin, Zhu, Weiping

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.19 MB

english, 2013

14

Caffeic acid derivatives: A new type of influenza neuraminidase inhibitors

Xie, Yuanchao, Huang, Bing, Yu, Kexiang, Shi, Fangyuan, Liu, Tianqi, Xu, Wenfang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 725 KB

english, 2013

15

Synthesis and preliminary evaluation steroidal antiestrogen–geldanamycin conjugates

Adam Hendricks, J., Hanson, Robert N., Amolins, Michael, Mihelcic, John M., Blagg, Brian S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 588 KB

english, 2013

16

3-Anhydro-6-hydroxy-ophiobolin A, a new sesterterpene inhibiting the growth of methicillin-resistant Staphylococcus aureus and inducing the cell death by apoptosis on K562, from the phytopathogenic fungus Bipolaris oryzae

Wang, Quan-Xin, Yang, Jian-Ling, Qi, Qiu-Yue, Bao, Li, Yang, Xiao-Li, Liu, Miao-Miao, Huang, Pei, Zhang, Li-Xin, Chen, Ji-Long, Cai, Lei, Liu, Hong-Wei

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 971 KB

english, 2013

17

A bioassay-driven discovery of an unexpected selenophene and its cytotoxicity

Csuk, René, Siewert, Bianka, Wiemann, Jana

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 971 KB

english, 2013

18

Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension

Bauman, David R., Whitehead, Alan, Contino, Lisa C., Cui, Jisong, Garcia-Calvo, Margarita, Gu, Xin, Kevin, Nancy, Ma, Xiuying, Pai, Lee-yuh, Shah, Kashmira, Shen, Xiaolan, Stribling, Sloan, Zokian, Hr

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 517 KB

english, 2013

19

8-Aminoquinoline-based ratiometric zinc probe: Unexpected binding mode and its application in living cells

Zhang, Liangwei, Cui, Xuemei, Sun, Jinyu, Wang, Yuli, Li, Weishuang, Fang, Jianguo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1018 KB

english, 2013

20

New azole antagonists with high affinity for the P2Y1 receptor

Ruel, Réjean, L’Heureux, Alexandre, Thibeault, Carl, Daris, Jean-Paul, Martel, Alain, Price, Laura A., Wu, Qimin, Hua, Ji, Wexler, Ruth R., Rehfuss, Robert, Lam, Patrick Y.S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.38 MB

english, 2013

21

Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase

Alafeefy, Ahmed M., Isik, Semra, Al-Jaber, Nabila A., Vullo, Daniela, Abdel-Aziz, Hatem A., Ashour, Abdelkader E., Awaad, Amani S., Capasso, Clemente, Supuran, Claudiu T.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.00 MB

english, 2013

22

A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain

Hoyt, Scott B., London, Clare, Abbadie, Catherine, Felix, John P., Garcia, Maria L., Jochnowitz, Nina, Karanam, Bindhu V., Li, Xiaohua, Lyons, Kathryn A., McGowan, Erin, Priest, Birgit T., Smith, McHa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 914 KB

english, 2013

23

Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase

Thalji, Reema K., McAtee, Jeff J., Belyanskaya, Svetlana, Brandt, Martin, Brown, Gregory D., Costell, Melissa H., Ding, Yun, Dodson, Jason W., Eisennagel, Steve H., Fries, Rusty E., Gross, Jeffrey W.,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 819 KB

english, 2013

24

Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A

DeGoey, David A., Betebenner, David A., Grampovnik, David J., Liu, Dachun, Pratt, John K., Tufano, Michael D., He, Wenping, Krishnan, Preethi, Pilot-Matias, Tami J., Marsh, Kennan C., Molla, Akhteruzz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 350 KB

english, 2013

25

Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1

Hurley, Christopher A., Blair, Wade S., Bull, Richard J., Chang, Christine, Crackett, Peter H., Deshmukh, Gauri, Dyke, Hazel J., Fong, Rina, Ghilardi, Nico, Gibbons, Paul, Hewitt, Peter R., Johnson, A

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.23 MB

english, 2013

26

A convenient synthesis of GDP-d-rhamnose: The donor substrate for d-rhamnosyltransferase WbpZ from Pseudomonas aeruginosa PAO1

Wang, Shuo, Tanaka, Hidenori, Hindsgaul, Ole, Lam, Joseph S., Brockhausen, Inka

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 883 KB

english, 2013

27

Synthesis of 7-oxabicyclo[2.2.1]hept-5-en-2-yl derivatives and their screening for antimicrobial and antioxidant properties

Dhanapal, Ramu, Perumal, Paramasivan T., Ramprasath, Chandrasekaran, Mathivanan, Narayanasamy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.46 MB

english, 2013

28

Juglone, isolated from Juglans mandshurica Maxim, induces apoptosis via down-regulation of AR expression in human prostate cancer LNCaP cells

Xu, Huali, Yu, Xiaofeng, Qu, Shaochun, Sui, Dayun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.13 MB

english, 2013

29

Ligand-inducible formation of RNA pseudoknot

Matsumoto, Saki, Hong, Changfeng, Otabe, Takahiro, Murata, Asako, Nakatani, Kazuhiko

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 524 KB

english, 2013

30

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 30 KB

english, 2013

31

The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1

Amaning, Kwame, Lowinski, Maryse, Vallee, Francois, Steier, Valerie, Marcireau, Christophe, Ugolini, Antonio, Delorme, Cecile, Foucalt, Frédéric, McCort, Gary, Derimay, Nathalie, Andouche, Cyrielle, V

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.86 MB

english, 2013

32

Synthesis and evaluation of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane, and benzodioxaphosphininamine sulfides and related compounds as potential anti-malarial agents

Mara, Christine, Dempsey, Enda, Bell, Angus, Barlow, James W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 774 KB

english, 2013

33

Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides

Muench, Stephen P., Stec, Jozef, Zhou, Ying, Afanador, Gustavo A., McPhillie, Martin J., Hickman, Mark R., Lee, Patty J., Leed, Susan E., Auschwitz, Jennifer M., Prigge, Sean T., Rice, David W., McLeo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.08 MB

english, 2013

34

Corrigendum to “In silico identification of poly(ADP-ribose)polymerase-1 inhibitors and their chemosensitizing effects against cisplatin-resistant human gastric cancer cells” [Bioorg. Med. Chem. Lett. 23 (2013) 2642–2646]

Le, Tuong Vy Thi, Suh, Jee Hee, Kim, Nakjeong, Park, Hyun-Ju

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 180 KB

english, 2013

35

Phosphorylation of chloramphenicol by a recombinant protein Yhr2 from Streptomyces avermitilis MA4680

Rajesh, Thangamani, Sung, Changmin, Kim, Hyeonjeong, Song, Eunjung, Park, Hyung-Yeon, Jeon, Jong-Min, Yoo, Dongwon, Kim, Hyun Joong, Kim, Yong Hyun, Choi, Kwon-Young, Song, Kyung-Guen, Yang, Yung-Hun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.24 MB

english, 2013

36

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.90 MB

english, 2013

37

Corrigendum to “The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2” [Bioorg. Med. Chem. Lett. 23 (2013) 1870–1873]

Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Degnan, Andrew P., Jiang, Xiang-Jun, Macci, Robert, Mathias, Neil R., Moench, Paul, Pin, Sokhom S., Schartman, Ri

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 270 KB

english, 2013

38

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties

Gunzner-Toste, Janet, Zhao, Guiling, Bauer, Paul, Baumeister, Timm, Buckmelter, Alexandre J., Caligiuri, Maureen, Clodfelter, Karl H., Fu, Bang, Han, Bingsong, Ho, Yen-Ching, Kley, Nikolai, Liang, Xia

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 3.58 MB

english, 2013

39

Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor

Pathuri, Gopal, Thorpe, Jessica E., Disch, Bryan C., Bailey-Downs, Lora C., Ihnat, Michael A., Gali, Hariprasad

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 648 KB

english, 2013

40

Optimization of a novel potent and selective bacterial DNA helicase inhibitor scaffold from a high throughput screening hit

Li, Bing, Pai, Ramdas, Aiello, Daniel, Di, Ming, Barnes, Marjorie H., Peet, Norton P., Bowlin, Terry L., Moir, Donald T.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.63 MB

english, 2013

41

Aromatic glycosyl disulfide derivatives: Evaluation of their inhibitory activities against Trypanosoma cruzi

Gutiérrez, Bessy, Muñoz, Christian, Osorio, Luis, Fehér, Krisztina, Illyés, Tünde-Zita, Papp, Zsuzsa, Kumar, Ambati Ashok, Kövér, Katalin E., Sagua, Hernán, Araya, Jorge E., Morales, Patricio, Szilágy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 504 KB

english, 2013

42

Synthesis and antimycobacterial evaluation of N-substituted 5-chloropyrazine-2-carboxamides

Servusová, Barbora, Vobicková, Jana, Paterová, Pavla, Kubíček, Vladimír, Kuneš, Jiří, Doležal, Martin, Zitko, Jan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 350 KB

english, 2013

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