Volume 25; Issue 4

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Bioorganic & Medicinal Chemistry Letters
Volume 25; Issue 4

Bioorganic & Medicinal Chemistry Letters

Volume 25; Issue 4

1

Development of novel Asf1–H3/H4 inhibitors

Miknis, Greg F., Stevens, Sarah J., Smith, Luke E., Ostrov, David A., Churchill, Mair E.A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 741 KB

english, 2015

2

Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors

Yang, Hao, Murigi, Francis N., Wang, Zhijian, Li, Junfeng, Jin, Hongjun, Tu, Zhude

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 341 KB

english, 2015

3

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin

Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., am Ende, Christopher W., Evrard, Edelweiss, Efremov, Ivan, Kauffman, Gregory W., Stepan, Antonia F., Stiff, Cory M., Xie, Longfei, Bales, Ke

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 348 KB

english, 2015

4

Biofilm inhibition of linezolid-like Schiff bases: Synthesis, biological activity, molecular docking and in silico ADME prediction

Sangshetti, Jaiprakash N., Khan, Firoz A. Kalam, Patil, Rajendra H., Marathe, Sayali D., Gade, Wasudev N., Shinde, Devanand B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.04 MB

english, 2015

5

Synthesis and evaluation of NS5A inhibitors containing diverse heteroaromatic cores

Henderson, James A., Bilimoria, Darius, Bubenik, Monica, Cadilhac, Caroline, Cottrell, Kevin M., Denis, Francois, Dietrich, Evelyne, Ewing, Nigel, Falardeau, Guy, Giroux, Simon, L’Heureux, Lucille, Li

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1006 KB

english, 2015

6

Benzimidazole-containing HCV NS5A inhibitors: Effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency

Henderson, James A., Bilimoria, Darius, Bubenik, Monica, Cadilhac, Caroline, Cottrell, Kevin M., Dietrich, Evelyne, Denis, Francois, Ewing, Nigel, Falardeau, Guy, Giroux, Simon, Grey, Ronald, L’Heureu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 386 KB

english, 2015

7

Synthesis, antimicrobial activity and molecular docking of novel tetracyclic scaffolds incorporating a flavonoid framework with medium sized oxygen heterocycles

Dongamanti, Ashok, Aamate, Vikas Kumar, Devulapally, Mohan Gandhi, Gundu, Srinivas, Kotni, Meena Kumari, Manga, Vijjulatha, Balasubramanian, Sridhar, Ernala, Prasad

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 728 KB

english, 2015

8

6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists

Sun, Wei, Kim, Hyo-Shin, Lee, Sunho, Jung, Aeran, Kim, Sung-Eun, Ann, Jihyae, Yoon, Suyoung, Choi, Sun, Lee, Jin Hee, Blumberg, Peter M., Frank-Foltyn, Robert, Bahrenberg, Gregor, Schiene, Klaus, Stoc

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 794 KB

english, 2015

9

Synthesis and membrane-protective activity of novel derivatives of α-mangostin at the C-4 position

Buravlev, Evgeny V., Shevchenko, Oksana G., Kutchin, Aleksandr V.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 630 KB

english, 2015

10

6-(Azaindol-2-yl)pyridine-3-sulfonamides as potent and selective inhibitors targeting hepatitis C virus NS4B

Chen, Guangming, Ren, Hongyu, Zhang, Nanjing, Lennox, William, Turpoff, Anthony, Paget, Steven, Li, Chunshi, Almstead, Neil, Njoroge, F. George, Gu, Zhengxian, Graci, Jason, Jung, Stephen P., Colacino

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 383 KB

english, 2015

11

The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors

Wurz, Ryan P., Pettus, Liping H., Jackson, Claire, Wu, Bin, Wang, Hui-Ling, Herberich, Brad, Cee, Victor, Lanman, Brian A., Reed, Anthony B., Chavez, Frank, Nixey, Thomas, Laszlo, Jimmy, Wang, Paul, N

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 934 KB

english, 2015

12

Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors

Wu, Bin, Wang, Hui-Ling, Cee, Victor J., Lanman, Brian A., Nixey, Thomas, Pettus, Liping, Reed, Anthony B., Wurz, Ryan P., Guerrero, Nadia, Sastri, Christine, Winston, Jeff, Lipford, J. Russell, Lee,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 616 KB

english, 2015

13

The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors

Wang, Hui-Ling, Cee, Victor J., Chavez, Frank, Lanman, Brian A., Reed, Anthony B., Wu, Bin, Guerrero, Nadia, Lipford, J. Russell, Sastri, Christine, Winston, Jeff, Andrews, Kristin L., Huang, Xin, Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 976 KB

english, 2015

14

The cryptophycins as potent payloads for antibody drug conjugates

Verma, Vishal A., Pillow, Thomas H., DePalatis, Laura, Li, Guangmin, Phillips, Gail Lewis, Polson, Andrew G., Raab, Helga E., Spencer, Susan, Zheng, Bing

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 459 KB

english, 2015

15

Synthesis and photophysical characterization of quasi push–pull dicyanodibenzodioxins and their anti-tumor activity against glioma cell line C6

Banerjee, Subhadeep, Chattopadhyay, Anjan, Banerjee, Arnab, Haridas, Meera, Saini, Praveen, Das, Moitreyi, Majik, Mahesh S., Maurya, Yogesh Kr.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 575 KB

english, 2015

16

Dithiocarbamate–thiourea hybrids useful as vaginal microbicides also show reverse transcriptase inhibition: Design, synthesis, docking and pharmacokinetic studies

Bala, Veenu, Jangir, Santosh, Mandalapu, Dhanaraju, Gupta, Sonal, Chhonker, Yashpal S., Lal, Nand, Kushwaha, Bhavana, Chandasana, Hardik, Krishna, Shagun, Rawat, Kavita, Maikhuri, Jagdamba P., Bhatta,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.74 MB

english, 2015

17

Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD

Digiacomo, Maria, Chen, Ziwei, Wang, Shengnan, Lapucci, Annalina, Macchia, Marco, Yang, Xiaohong, Chu, Jiaqi, Han, Yifan, Pi, Rongbiao, Rapposelli, Simona

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 713 KB

english, 2015

18

Iminosugars as a new class of cholinesterase inhibitors

Decroocq, Camille, Stauffert, Fabien, Pamlard, Olivier, Oulaïdi, Farah, Gallienne, Estelle, Martin, Olivier R., Guillou, Catherine, Compain, Philippe

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 938 KB

english, 2015

19

Synthesis and properties of vitamin E analog-conjugated neomycin for delivery of RNAi drugs to liver cells

Iwata, Rintaro, Nakayama, Futoshi, Hirochi, Sakie, Sato, Kazuki, Piao, Wenying, Nishina, Kazutaka, Yokota, Takanori, Wada, Takeshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 963 KB

english, 2015

20

Insights on the role of boron containing moieties in the design of new potent and efficient agonists targeting the β2 adrenoceptor

Soriano-Ursúa, Marvin A., Arias-Montaño, José A., Correa-Basurto, José, Hernández-Martínez, Christian F., López-Cabrera, Yessica, Castillo-Hernández, Maria C., Padilla-Martínez, Itzia I., Trujillo-Fer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.38 MB

english, 2015

21

Computer-aided identification of novel anticancer compounds with a possible dual HER1/HER2 inhibition mechanism

Elseginy, Samia A., Lazaro, Glorianne, Nawwar, Galal A.M., Amin, Kamilia M., Hiscox, Stephen, Brancale, Andrea

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 751 KB

english, 2015

22

Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists

Sasmal, Pradip K., Krishna, C. Vamsee, Adabala, S. Sudheerkumar, Roshaiah, M., Rawoof, Khaji Abdul, Thadi, Emima, Sukumar, K. Pavan, Cheera, Srisailam, Abbineni, Chandrasekhar, Rao, K.V.L. Narasimha,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.21 MB

english, 2015

23

Synthesis and transmembrane anion/cation symport activity of a rigid bis(choloyl) conjugate functionalized with guanidino groups

Deng, Li-Qun, Li, Zhi, Lu, Yong-Ming, Chen, Jin-Xiang, Zhou, Chun-Qiong, Wang, Bo, Chen, Wen-Hua

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 646 KB

english, 2015

24

Design of novel CSA analogues as potential safeners and fungicides

Zheng, Yang, Liu, Bin, Gou, Zhaopin, Li, Yao, Zhang, Xiao, Wang, Yanqing, Yu, Shujing, Li, Yonghong, Sun, Dequn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 385 KB

english, 2015

25

Thiol-derivatized minihepcidins retain biological activity

Fung, Eileen, Chua, Kristine, Ganz, Tomas, Nemeth, Elizabeta, Ruchala, Piotr

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 523 KB

english, 2015

26

SAR-studies of γ-secretase modulators with PPARγ-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer’s disease

Flesch, Daniel, Ness, Julia, Lamers, Christina, Dehm, Friederike, Popella, Sven, Steri, Ramona, Ogorek, Isabella, Hieke, Martina, Dannhardt, Gerd, Werz, Oliver, Weggen, Sascha, Schubert-Zsilavecz, Man

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.66 MB

english, 2015

27

The combination of thioxodihydroquinazolinones and platinum drugs reverses platinum resistance in tumor cells by inducing mitochondrial apoptosis independent of Bax and Bak

Qian, Wei, Salamoun, Joseph, Wang, Jingnan, Roginskaya, Vera, Van Houten, Bennett, Wipf, Peter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.43 MB

english, 2015

28

A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase

Garro, Hugo A., García, Celina, Martín, Victor S., Tonn, Carlos E., Pungitore, Carlos R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 675 KB

english, 2015

29

Pyridine and pyridinone-based factor XIa inhibitors

Corte, James R., Fang, Tianan, Hangeland, Jon J., Friends, Todd J., Rendina, Alan R., Luettgen, Joseph M., Bozarth, Jeffrey M., Barbera, Frank A., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashanka

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.62 MB

english, 2015

30

Two new protein tyrosine phosphatase 1B inhibitors, hyattellactones A and B, from the Indonesian marine sponge Hyattella sp.

Abdjul, Delfly B., Yamazaki, Hiroyuki, Takahashi, Ohgi, Kirikoshi, Ryota, Mangindaan, Remy E.P., Namikoshi, Michio

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 554 KB

english, 2015

31

Novel synthetic coumarins that targets NF-κB in Hepatocellular carcinoma

Neelgundmath, Mahabaleshwaraiah, Dinesh, Koragere Rajashekar, Mohan, Chakrabhavi Dhananjaya, Li, Feng, Dai, Xiaoyun, Siveen, Kodappully Sivaraman, Paricharak, Shardul, Mason, Daniel J., Fuchs, Julian

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.68 MB

english, 2015

32

Inhibitory constituents of Sophora tonkinensis on nitric oxide production in RAW 264.7 macrophages

Lee, Jin Woo, Lee, Ji Hoon, Lee, Chul, Jin, Qinghao, Lee, Dongho, Kim, Youngsoo, Hong, Jin Tae, Lee, Mi Kyeong, Hwang, Bang Yeon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 383 KB

english, 2015

33

Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers

Giroux, Simon, Bilimoria, Darius, Cadilhac, Caroline, Cottrell, Kevin M., Denis, Francois, Dietrich, Evelyne, Ewing, Nigel, Henderson, James A., L’Heureux, Lucille, Mani, Nagraj, Morris, Mark, Nicolas

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 989 KB

english, 2015

34

The discovery of 1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 1

Bond, Silas, Draffan, Alistair G., Fenner, Jennifer E., Lambert, John, Lim, Chin Yu, Lin, Bo, Luttick, Angela, Mitchell, Jeffrey P., Morton, Craig J., Nearn, Roland H., Sanford, Vanessa, Stanislawski,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 4.10 MB

english, 2015

35

Prodrugs of imidazotriazine and pyrrolotriazine C-nucleosides can increase anti-HCV activity and enhance nucleotide triphosphate concentrations in vitro

Tyndall, Edward M., Draffan, Alistair G., Frey, Barbara, Pool, Brett, Halim, Rosliana, Jahangiri, Saba, Bond, Silas, Wirth, Veronika, Luttick, Angela, Tilmanis, Danielle, Thomas, Jesse, Porter, Kate,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 823 KB

english, 2015

36

1,2,3,9b-Tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 2: Identification of BTA9881 as a preclinical candidate

Bond, Silas, Draffan, Alistair G., Fenner, Jennifer E., Lambert, John, Lim, Chin Yu, Lin, Bo, Luttick, Angela, Mitchell, Jeffrey P., Morton, Craig J., Nearn, Roland H., Sanford, Vanessa, Anderson, Kel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.39 MB

english, 2015

37

Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators

Savall, Brad M., Meduna, Steven P., Tays, Kevin, Cai, Hui, Thurmond, Robin L., McGovern, Patricia, Gaul, Michael, Zhao, Bao-Ping, Edwards, James P.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 4.37 MB

english, 2015

38

Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: Non-symmetric inhibitors with potent activity against genotype 1a and 1b

Giroux, Simon, Bilimoria, Darius, Cadilhac, Caroline, Cottrell, Kevin M., Denis, Francois, Dietrich, Evelyne, Ewing, Nigel, Henderson, James A., L’Heureux, Lucille, Mani, Nagraj, Morris, Mark, Nicolas

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.49 MB

english, 2015

39

Thio- and selenoglycosides as ligands for biomedically relevant lectins: Valency–activity correlations for benzene-based dithiogalactoside clusters and first assessment for (di)selenodigalactosides

André, Sabine, Kövér, Katalin E., Gabius, Hans-Joachim, Szilágyi, László

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 797 KB

english, 2015

40

Structure–activity relationships of diverse ACGs against multidrug resistant human lung cancer cell line A549/Taxol

Yuan, Fei, Bai, Ganggang, Chen, Yong, Miao, Yunjie, Chen, Jianwei, Li, Xiang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 344 KB

english, 2015

41

Flavokawains B and C, melanogenesis inhibitors, isolated from the root of Piper methysticum and synthesis of analogs

Jeong, Hye-Jin, Lee, Chang Seok, Choi, Janggyoo, Hong, Yong Deog, Shin, Song Seok, Park, Jun Seong, Lee, John Hwan, Lee, Seokyong, Yoon, Kee Dong, Ko, Jaeyoung

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 387 KB

english, 2015

42

Multidrug resistance–reversal effects of resin glycosides from Dichondra repens

Song, Wei-bin, Wang, Wen-qiong, Zhang, Shu-wei, Xuan, Li-jiang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 364 KB

english, 2015

43

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease

Chen, Jian Jeffrey, Liu, Qingyian, Yuan, Chester, Gore, Vijay, Lopez, Patricia, Ma, Vu, Amegadzie, Albert, Qian, Wenyuan, Judd, Ted C., Minatti, Ana E., Brown, James, Cheng, Yuan, Xue, May, Zhong, Wen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.38 MB

english, 2015

44

Synthesis of oolongtheanins and their inhibitory activity on micellar cholesterol solubility in vitro

Ogawa, Kazuki, Hirose, Sayumi, Yamamoto, Hitomi, Shimada, Masaya, Nagaoka, Satoshi, Yanase, Emiko

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 542 KB

english, 2015

45

Evaluation of synthetic naphthalene derivatives as novel chemical chaperones that mimic 4-phenylbutyric acid

Mimori, Seisuke, Koshikawa, Yukari, Mashima, Yu, Mitsunaga, Katsuyoshi, Kawada, Koichi, Kaneko, Masayuki, Okuma, Yasunobu, Nomura, Yasuyuki, Murakami, Yasuoki, Kanzaki, Tetsuto, Hamana, Hiroshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 633 KB

english, 2015

46

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 3.52 MB

english, 2015

47

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 30 KB

english, 2015

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