Volume 24; Issue 5

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Bioorganic & Medicinal Chemistry Letters
Volume 24; Issue 5

Bioorganic & Medicinal Chemistry Letters

Volume 24; Issue 5

1

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: Part 2. Pyridazine-based analogs

Yang, Shyh-Ming, Tang, Yuting, Rano, Thomas, Lu, Huajun, Kuo, Gee-Hong, Gaul, Michael D., Li, Yaxin, Ho, George, Lang, Wensheng, Conway, James G., Liang, Yin, Lenhard, James M., Demarest, Keith T., Mu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 602 KB

english, 2014

2

Targeted amplification of delivery to cell surface receptors by dendrimer self-assembly

Isaacman, Steven, Buckley, Michael, Wang, Xiaojian, Wang, Edwin Y., Liebes, Leonard, Canary, James W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 364 KB

english, 2014

3

A facile access to novel steroidal 17-2′-(1′,3′,4′)-oxadiazoles, and an evaluation of their cytotoxic activities in vitro

Kovács, Dóra, Mótyán, Gergő, Wölfling, János, Kovács, Ida, Zupkó, István, Frank, Éva

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 336 KB

english, 2014

4

Syntheses and structure–activity relationships for some triazolyl p38α MAPK inhibitors

Seerden, Jean-Paul G., Leusink-Ionescu, Gabriela, Leguijt, Robin, Saccavini, Catherine, Gelens, Edith, Dros, Bas, Woudenberg-Vrenken, Titia, Molema, Grietje, Kamps, Jan A.A.M., Kellogg, Richard M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.61 MB

english, 2014

5

Synthesis of novel 5-(3-alkylquinolin-2-yl)-3-aryl isoxazole derivatives and their cytotoxic activity

Sambasiva Rao, P., Kurumurthy, C., Veeraswamy, B., Poornachandra, Y., Ganesh Kumar, C., Narsaiah, B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 367 KB

english, 2014

6

3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor

Lee, Younho, Shin, Yong June, Ahn, Soon Kil

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.16 MB

english, 2014

7

Switching cannabinoid response from CB2 agonists to FAAH inhibitors

Tourteau, Aurélien, Leleu-Chavain, Natascha, Body-Malapel, Mathilde, Andrzejak, Virginie, Barczyk, Amélie, Djouina, Madjid, Rigo, Benoit, Desreumaux, Pierre, Chavatte, Philippe, Millet, Régis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 701 KB

english, 2014

8

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

Keith, John M., Hawryluk, Natalie, Apodaca, Richard L., Chambers, Allison, Pierce, Joan M., Seierstad, Mark, Palmer, James A., Webb, Michael, Karbarz, Mark J., Scott, Brian P., Wilson, Sandy J., Luo,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.94 MB

english, 2014

9

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase

Evenäs, Johan, Edfeldt, Fredrik, Lepistö, Matti, Svitacheva, Naila, Synnergren, Anna, Lundquist, Britta, Gränse, Mia, Rönnholm, Anna, Varga, Mikael, Wright, John, Wei, Min, Yue, Sherrie, Wang, Junfeng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.09 MB

english, 2014

10

Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway

Cros, Cécile D., Toth, Istvan, Blanchfield, Joanne T.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 296 KB

english, 2014

11

Rugulactone derivatives act as inhibitors of NF-κB activation and modulates the transcription of NF-κB dependent genes in MDA-MB-231cells

Mohapatra, Debendra K., Reddy, D. Sai, Janaki Ramaiah, M., Ghosh, Sowjanya, Pothula, Vikram, Lunavath, Swetha, Thomas, Shine, Pushpa Valli, S.N.C.V.L., Bhadra, Manika Pal, Yadav, Jhillu S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.23 MB

english, 2014

12

6-Triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrases IX and XII

Grandane, Aiga, Tanc, Muhammet, Zalubovskis, Raivis, Supuran, Claudiu T.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 426 KB

english, 2014

13

Synthesis and in vivo evaluation of N-ethylamino-2-oxo-1,2-dihydro-quinoline-3-carboxamide for inhibition of intestinal tumorigenesis in APCMin/+ mice

Pathuri, Gopal, Li, Qian, Mohammed, Altaf, Gali, Hariprasad, Pento, J. Thomas, Rao, Chinthalapally V.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 661 KB

english, 2014

14

Synthesis and biological evaluation of new boron-containing chlorin derivatives as agents for both photodynamic therapy and boron neutron capture therapy of cancer

Asano, Ryuji, Nagami, Amon, Fukumoto, Yuki, Miura, Kaori, Yazama, Futoshi, Ito, Hideyuki, Sakata, Isao, Tai, Akihiro

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 555 KB

english, 2014

15

Corrigendum to “Identification through structure-based methods of a bacterial NAD+-dependent DNA ligase inhibitor that avoids known resistance mutations” [Bioorg. Med. Chem. Lett. 24 (2014) 360–366]

Murphy-Benenato, Kerry, Wang, Hongming, McGuire, Helen M., Davis, Hajnalka E., Gao, Ning, Bryan Prince, D., Jahic, Haris, Stokes, Suzanne S., Ann Boriack-Sjodin, P.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 491 KB

english, 2014

16

Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIα by its cytotoxic β-carboline alkaloids

de Oliveira Figueiredo, Patrícia, Perdomo, Renata Trentin, Garcez, Fernanda Rodrigues, de Fatima Cepa Matos, Maria, de Carvalho, João Ernesto, Garcez, Walmir Silva

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 474 KB

english, 2014

17

Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M1 positive allosteric modulators

Kuduk, Scott D., Di Marco, Christina N., Saffold, Jonathan R., Ray, William J., Ma, Lei, Wittmann, Marion, Koeplinger, Kenneth A., Thompson, Charles D., Hartman, George D., Bilodeau, Mark T., Beshore,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.24 MB

english, 2014

18

A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox

Kamogawa, Erisa, Sueishi, Yoshimi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 517 KB

english, 2014

19

Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity

Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 582 KB

english, 2014

20

Identification of diverse natural products as falcipain-2 inhibitors through structure-based virtual screening

Wang, Liyan, Zhang, Shoude, Zhu, Junsheng, Zhu, Lili, Liu, Xiaofeng, Shan, Lei, Huang, Jin, Zhang, Weidong, Li, Honglin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 693 KB

english, 2014

21

Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

Olsson, Roine I., Jacobson, Ingemar, Iliefski, Tommy, Boström, Jonas, Davidsson, Öjvind, Fjellström, Ola, Björe, Annika, Olsson, Christina, Sundell, Johan, Gran, Ulrik, Gyll, Jonna, Malmberg, Jesper,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.06 MB

english, 2014

22

Antifungal ether diglycosides from Matayba guianensis Aublet

de Assis, Polyana A., Theodoro, Phellipe N.E.T., de Paula, José E., Araújo, Ana J., Costa-Lotufo, Letícia V., Michel, Sylvie, Grougnet, Raphaël, Kritsanida, Marina, Espindola, Laila S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 291 KB

english, 2014

23

MHY884, a newly synthesized tyrosinase inhibitor, suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress

Choi, Yeon Ja, Uehara, Yohei, Park, Ji Young, Kim, Seong Jin, Kim, So Ra, Lee, Hee Won, Moon, Hyung Ryong, Chung, Hae Young

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 996 KB

english, 2014

24

Synthesis and biological evaluation of baicalein derivatives as potent antitumor agents

Luo, Rong, Wang, Jubo, Zhao, Li, Lu, Na, You, Qidong, Guo, Qinglong, Li, Zhiyu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1014 KB

english, 2014

25

Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists

Wu, Tian-Ming, Wang, Dao-Cai, Xiang, Pu, Zhang, Jian-Nan, Sang, Ya-Xiong, Lin, Hong-Jun, Chen, Jie, Xie, Gang, Song, Hang, Zhao, Ying-Lan, Xie, Yong-Mei

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.99 MB

english, 2014

26

Lipoxygenase inhibitors derived from marine macroalgae

Kurihara, Hideyuki, Kagawa, Yoshio, Konno, Remi, Kim, Sang Moo, Takahashi, Koretaro

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 338 KB

english, 2014

27

Psoralidin, a coumestan analogue, as a novel potent estrogen receptor signaling molecule isolated from Psoralea corylifolia

Liu, Xiyuan, Nam, Joo-Won, Song, Yun Seon, Viswanath, Ambily Nath Indu, Pae, Ae Nim, Kil, Yun-Seo, Kim, Hee-Doo, Park, Jong Hoon, Seo, Eun-Kyoung, Chang, Minsun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 601 KB

english, 2014

28

Identification of 1-{2-[4-chloro-1′-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4′-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y1 antagonist as an antiplatelet agent

Jeon, Yoon T., Yang, Wu, Qiao, Jennifer X., Li, Ling, Ruel, Rejean, Thibeault, Carl, Hiebert, Sheldon, Wang, Tammy C., Wang, Yufeng, Liu, Yajun, Clark, Charles G., Wong, Henry S., Zhu, Juliang, Wu, Da

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.21 MB

english, 2014

29

Substituted benzene sulfonamides incorporating 1,3,5-triazinyl moieties potently inhibit human carbonic anhydrases II, IX and XII

Saluja, Amrita K., Tiwari, Meena, Vullo, Daniela, Supuran, Claudiu T.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 745 KB

english, 2014

30

Discovery of 2-(1H-indazol-1-yl)-thiazole derivatives as selective EP1 receptor antagonists for treatment of overactive bladder by core structure replacement

Atobe, Masakazu, Naganuma, Kenji, Kawanishi, Masashi, Morimoto, Akifumi, Kasahara, Ken-ichi, Ohashi, Shigeki, Suzuki, Hiroko, Hayashi, Takahiko, Miyoshi, Shiro

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.52 MB

english, 2014

31

Lead optimization of HMBA to develop potent HEXIM1 inducers

Zhong, Bo, Lama, Rati, Ketchart, Wannarasmi, Montano, Monica M., Su, Bin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 857 KB

english, 2014

32

Identification and biological evaluation of flavonoids from the fruits of Prunus mume

Yan, Xi-Tao, Li, Wei, Sun, Ya-Nan, Yang, Seo-Young, Lee, Sang-Hyun, Chen, Jian-Bo, Jang, Hae-Dong, Kim, Young-Ho

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 500 KB

english, 2014

33

Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of α-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum

Weldon, David J., Shah, Falgun, Chittiboyina, Amar G., Sheri, Anjaneyulu, Chada, Raji Reddy, Gut, Jiri, Rosenthal, Philip J., Shivakumar, Develeena, Sherman, Woody, Desai, Prashant, Jung, Jae-Chul, Av

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.51 MB

english, 2014

34

p-Terphenyl O-β-glucuronides, DNA topoisomerase inhibitors from Streptomyces sp. LZ35ΔgdmAI

Deng, Jingjing, Lu, Chunhua, Li, Shanren, Hao, Huilin, Li, Zhenyu, Zhu, Jing, Li, Yaoyao, Shen, Yuemao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 733 KB

english, 2014

35

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.47 MB

english, 2014

36

Identification of malic enzyme mutants depending on 1,2,3-triazole moiety-containing nicotinamide adenine dinucleotide analogs

Hou, Shuhua, Ji, Debin, Liu, Wujun, Wang, Lei, Zhao, Zongbao (Kent)

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 391 KB

english, 2014

37

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 30 KB

english, 2014

38

The survival times of malaria-infected mice are prolonged more by several new two-carbon-linked artemisinin-derived dimer carbamates than by the trioxane antimalarial drug artemether

Conyers, Ryan C., Mazzone, Jennifer R., Siegler, Maxime A., Tripathi, Abhai K., Sullivan, David J., Mott, Bryan T., Posner, Gary H.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 768 KB

english, 2014

39

A radiogallium–DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging

Sano, Kohei, Masuda, Ryo, Hisada, Hayato, Oishi, Shinya, Shimokawa, Kenta, Ono, Masahiro, Fujii, Nobutaka, Saji, Hideo, Mukai, Takahiro

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 416 KB

english, 2014

40

4′-Substituted pyrimidine nucleosides lacking 5′-hydroxyl function as potential anti-HCV agents

Shakya, Neeraj, Vedi, Satish, Liang, Chao, Yang, Fang, Agrawal, Babita, Kumar, Rakesh

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 624 KB

english, 2014

41

Inhibition of glutamate racemase by substrate–product analogues

Pal, Mohan, Bearne, Stephen L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1020 KB

english, 2014

42

Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide

Bhat, Mashooq Ahmad, Khan, Abdul Arif, Khan, Shahanavaj, Al-Omar, Mohamed A., Parvez, Mohammad Khalid, Al-Dosari, Mohammed Salem, Al-Dhfyan, Abdullah

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 475 KB

english, 2014

43

Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines

Reddy Chamakura, Upendar, Sailaja, E., Dulla, Balakrishna, Kalle, Arunasree M., Bhavani, S., Rambabu, D., Kapavarapu, Ravikumar, Rao, M.V. Basaveswara, Pal, Manojit

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.35 MB

english, 2014

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