Volume 25; Issue 5

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Bioorganic & Medicinal Chemistry Letters
Volume 25; Issue 5

Bioorganic & Medicinal Chemistry Letters

Volume 25; Issue 5

1

Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity

Beaulieu, Pierre L., Bolger, Gordon, Deon, Dan, Duplessis, Martin, Fazal, Gulrez, Gagnon, Alexandre, Garneau, Michel, LaPlante, Steven, Stammers, Timothy, Kukolj, George, Duan, Jianmin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 376 KB

english, 2015

2

Aza follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 1: Mitigating the genotoxic liability of an aniline metabolite

Beaulieu, Pierre L., Bolger, Gordon, Duplessis, Martin, Gagnon, Alexandre, Garneau, Michel, Stammers, Timothy, Kukolj, George, Duan, Jianmin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 505 KB

english, 2015

3

Design and synthesis of novel 1,2,3-triazole–pyrimidine–urea hybrids as potential anticancer agents

Ma, Li-Ying, Wang, Bo, Pang, Lu-Ping, Zhang, Miao, Wang, Sai-Qi, Zheng, Yi-Chao, Shao, Kun-Peng, Xue, Deng-Qi, Liu, Hong-Min

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 535 KB

english, 2015

4

Synthesis and SAR study of potent and selective PI3Kδ inhibitors

Bui, Minna, Hao, Xiaolin, Shin, Youngsook, Cardozo, Mario, He, Xiao, Henne, Kirk, Suchomel, Julia, McCarter, John, McGee, Lawrence R., San Miguel, Tisha, Medina, Julio C., Mohn, Deanna, Tran, Thuy, Wa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 440 KB

english, 2015

5

Design of new hybrid template by linking quinoline, triazole and dihydroquinoline pharmacophoric groups: A greener approach to novel polyazaheterocycles as cytotoxic agents

Praveena, Koduru Sri Shanthi, Shivaji Ramarao, Edupuganti Veera Venkat, Murthy, Nandula Yadagiri Sreenivasa, Akkenapally, Surekha, Ganesh Kumar, C., Kapavarapu, Ravikumar, Pal, Sarbani

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.39 MB

english, 2015

6

Biosynthesis of human diazepam and clonazepam metabolites

de Paula, Núbia C., Araujo Cordeiro, Kelly C.F., de Melo Souza, Paula L., Nogueira, Diogo F., da Silva e Sousa, Diego B., Costa, Maísa B., Noël, François, de Oliveira, Valéria

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 709 KB

english, 2015

7

Target Engagement in Lead Generation

Durham, Timothy B., Blanco, Maria-Jesus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.61 MB

english, 2015

8

Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro

Guo, Feng-Jiao, Sun, Juan, Gao, Li-Li, Wang, Xin-Yi, Zhang, Yang, Qian, Shao-Song, Zhu, Hai-Liang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 906 KB

english, 2015

9

Antibody-integrated and functionalized graphite-encapsulated magnetic beads, produced using ammonia gas plasma technology, for capturing Salmonella

Sakudo, Akikazu, Chou, Han, Nagatsu, Masaaki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.49 MB

english, 2015

10

Constituents of the stem barks of Ailanthus altissima and their potential to inhibit LPS-induced nitric oxide production

Kim, Hye Mi, Kim, Su Jung, Kim, Ha-Yeong, Ryu, Byeol, Kwak, Hokwang, Hur, Jonghyun, Choi, Jung-Hye, Jang, Dae Sik

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 425 KB

english, 2015

11

Transporter-mediated tissue targeting of therapeutic molecules in drug discovery

Zhou, Jingye, Xu, Jianfeng, Huang, Zheng, Wang, Minmin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 852 KB

english, 2015

12

Improving the dissolution and bioavailability of 6-mercaptopurine via co-crystallization with isonicotinamide

Wang, Jian-Rong, Yu, Xueping, Zhou, Chun, Lin, Yunfei, Chen, Chen, Pan, Guoyu, Mei, Xuefeng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 987 KB

english, 2015

13

Schiff’s bases of quinazolinone derivatives: Synthesis and SAR studies of a novel series of potential anti-inflammatory and antioxidants

Rakesh, K.P., Manukumar, H.M., Gowda, D. Channe

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.82 MB

english, 2015

14

Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents

Kumari, Shikha, Mishra, Chandra Bhushan, Tiwari, Manisha

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 948 KB

english, 2015

15

Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat

Tran, Thuy-Anh, Shin, Young-Jun, Kramer, Bryan, Choi, Juyi, Zou, Ning, Vallar, Pureza, Martens, Peter, Douglas Boatman, P., Adams, John W., Ramirez, Juan, Shi, Yunqing, Morgan, Michael, Unett, David J

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 657 KB

english, 2015

16

Synthesis and in vitro evaluation of novel 8-aminoquinoline–pyrazolopyrimidine hybrids as potent antimalarial agents

Kannan, Murugan, Raichurkar, Anandkumar V., Khan, Fazlur Rahman Nawaz, Iyer, Pravin S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.30 MB

english, 2015

17

Synthesis and characterization of 1′-C-cyano-2′-fluoro-2′-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors

Kirschberg, Thorsten A., Mish, Michael R., Zhang, Lijun, Squires, Neil H., Wang, Ke-Yu, Cho, Aesop, Feng, Joy Y., Fenaux, Martijn, Babusis, Darius, Park, Yeojin, Ray, Adrian S., Kim, Choung U.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.35 MB

english, 2015

18

Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3β inhibitors for Alzheimer’s disease

Fukunaga, Kenji, Sakai, Daiki, Watanabe, Kazutoshi, Nakayama, Kazuki, Kohara, Toshiyuki, Tanaka, Hiroshi, Sunada, Shinji, Nabeno, Mika, Okamoto, Masako, Saito, Ken-Ichi, Eguchi, Jun-ichi, Mori, Akiko,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.41 MB

english, 2015

19

Quantification of proteins using 13C7-labeled and unlabeled iodoacetanilide by nano liquid chromatography/nanoelectrospray ionization and by selected reaction monitoring mass spectrometry

Kurono, Sadamu, Kaneko, Yuka, Matsuura, Shuji, Niwayama, Satomi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.06 MB

english, 2015

20

Discovery of non-electrophilic capsaicinoid-type TRPA1 ligands

Del Prete, Danilo, Caprioglio, Diego, Appendino, Giovanni, Minassi, Alberto, Schiano-Moriello, Aniello, Di Marzo, Vincenzo, De Petrocellis, Luciano

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 460 KB

english, 2015

21

BPIC: A novel anti-tumor lead capable of inhibiting inflammation and scavenging free radicals

Li, Shan, Wang, Yuji, Zhao, Ming, Wu, Jianhui, Peng, Shiqi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.48 MB

english, 2015

22

Chemopreventive flavonoids from Millettia pulchra Kurz var-laxior (Dunn) Z.Wei (Yulangsan) function as Michael reaction acceptors

Wang, Wenli, Wang, Jian, Li, Ning, Zhang, Xiangrong, Zhao, Weihong, Li, Jiayuan, Si, Yingying

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 697 KB

english, 2015

23

11C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

Andersen, Valdemar L., Hansen, Hanne D., Herth, Matthias M., Dyssegaard, Agnete, Knudsen, Gitte M., Kristensen, Jesper L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 743 KB

english, 2015

24

Synthesis of benzopentathiepin analogs and their evaluation as inhibitors of the phosphatase STEP

Baguley, Tyler D., Nairn, Angus C., Lombroso, Paul J., Ellman, Jonathan A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 723 KB

english, 2015

25

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase

Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Che

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.38 MB

english, 2015

26

Novel 64Cu-radiolabeled bile acid conjugates for targeted PET imaging

Chong, Hyun-Soon, Chen, Yunwei, Kang, Chi Soo, Sun, Xiang, Wu, Ningjie

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 642 KB

english, 2015

27

Anti-inflammatory activity of phenolic compounds from the whole plant of Scutellaria indica

Cuong, To Dao, Hung, Tran Manh, Lee, Joo-Sang, Weon, Kwon-Yeon, Woo, Mi Hee, Min, Byung Sun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 592 KB

english, 2015

28

Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase

Gritzalis, Dimitrios, Park, Jaeok, Chiu, Wei, Cho, Hyungjun, Lin, Yih-Shyan, De Schutter, Joris W., Lacbay, Cyrus M., Zielinski, Michal, Berghuis, Albert M., Tsantrizos, Youla S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.04 MB

english, 2015

29

Further studies on anti-invasive chemotypes: An excursion from chalcones to curcuminoids

Roman, Bart I., De Ryck, Tine, Verhasselt, Sigrid, Bracke, Marc E., Stevens, Christian V.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.69 MB

english, 2015

30

Marine natural products as inhibitors of cystathionine beta-synthase activity

Thorson, Megan K., Van Wagoner, Ryan M., Harper, Mary Kay, Ireland, Chris M., Majtan, Tomas, Kraus, Jan P., Barrios, Amy M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 548 KB

english, 2015

31

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

File:

PDF, 2.52 MB

2015

32

Corrigendum to “(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors” [Bioorg. Med. Chem. Lett. 15 (2005) 3402–3406]

Bamford, Mark J., Alberti, Michael J., Bailey, Nicholas, Davies, Susannah, Dean, David K., Gaiba, Alessandra, Garland, Stephen, Harling, John D., Jung, David K., Panchal, Terence A., Parr, Christopher

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 248 KB

english, 2015

33

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 30 KB

english, 2015