Volume 23; Issue 4

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Bioorganic & Medicinal Chemistry Letters
Volume 23; Issue 4

Bioorganic & Medicinal Chemistry Letters

Volume 23; Issue 4

1

Synthesis and antibacterial evaluation of a novel tricyclic oxaborole-fused fluoroquinolone

Li, Xianfeng, Zhang, Yong-Kang, Plattner, Jacob J., Mao, Weimin, Alley, M.R.K., Xia, Yi, Hernandez, Vincent, Zhou, Yasheen, Ding, Charles Z., Li, Jinpeng, Shao, Zhijun, Zhang, Hongwei, Xu, Musheng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 488 KB

english, 2013

2

Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency

Bollini, Mariela, Gallardo-Macias, Ricardo, Spasov, Krasimir A., Tirado-Rives, Julian, Anderson, Karen S., Jorgensen, William L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 661 KB

english, 2013

3

Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors

Ye, Xiaocong M., Konradi, Andrei W., Sun, Minghua, Yuan, Shendong, Aubele, Danielle L., Dappen, Michael, Dressen, Darren, Garofalo, Albert W., Jagodzinski, Jacek J., Latimer, Lee, Probst, Gary D., Sha

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 703 KB

english, 2013

4

Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Powell, Noel A., Hoffman, Jennifer K., Ciske, Fred L., Kohrt, Jeffrey T., Baxi, Sangita M., Peng, Yun-Wen, Zhong, Min, Catana, Cornel, Ohren, Jeff, Perrin, Lisa A., Edmunds, Jeremy J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 372 KB

english, 2013

5

The first total synthesis and biological evaluation of marine natural products ma’edamines A and B

Saha, Sanjay, Venkata Ramana Reddy, Ch., Chiranjeevi, T., Addepally, Uma, Chinta Rao, T.S., Patro, Balaram

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.14 MB

english, 2013

6

A novel series of N-(azetidin-3-yl)-2-(heteroarylamino)acetamide CCR2 antagonists

Subasinghe, Nalin L., Lanter, James, Markotan, Thomas, Opas, Evan, McKenney, Sandra, Crysler, Carl, Hou, Cuifen, O’Neill, John, Johnson, Dana, Sui, Zhihua

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.53 MB

english, 2013

7

Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation

Arhancet, Graciela B., Walker, Daniel P., Metz, Sue, Fobian, Yvette M., Heasley, Steven E., Carter, Jeffrey S., Springer, John R., Jones, Darin E., Hayes, Michael J., Shaffer, Alexander F., Jerome, Gi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.23 MB

english, 2013

8

Cardioprotective potential of N,α-l-rhamnopyranosyl vincosamide, an indole alkaloid, isolated from the leaves of Moringa oleifera in isoproterenol induced cardiotoxic rats: In vivo and in vitro studies

Panda, Sunanda, Kar, Anand, Sharma, Pratibha, Sharma, Ashok

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 547 KB

english, 2013

9

Phthalazinone inhibitors of inosine-5′-monophosphate dehydrogenase from Cryptosporidium parvum

Johnson, Corey R., Gorla, Suresh Kumar, Kavitha, Mandapati, Zhang, Minjia, Liu, Xiaoping, Striepen, Boris, Mead, Jan R., Cuny, Gregory D., Hedstrom, Lizbeth

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 592 KB

english, 2013

10

Synthesis and dual biological effects of hydroxycinnamoyl phenylalanyl/prolyl hydroxamic acid derivatives as tyrosinase inhibitor and antioxidant

Kwak, Seon-Yeong, Yang, Jin-Kyoung, Choi, Hye-Ryung, Park, Kyung-Chan, Kim, Young-Bu, Lee, Yoon-Sik

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 720 KB

english, 2013

11

Discovery of a small-molecule antiviral targeting the HIV-1 matrix protein

Zentner, Isaac, Sierra, Luz-Jeannette, Maciunas, Lina, Vinnik, Andrei, Fedichev, Peter, Mankowski, Marie K., Ptak, Roger G., Martín-García, Julio, Cocklin, Simon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 413 KB

english, 2013

12

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Powell, Noel A., Hoffman, Jennifer K., Ciske, Fred L., Kaufman, Michael D., Kohrt, Jeffrey T., Quin, John, Sheehan, Derek J., Delaney, Amy, Baxi, Sangita M., Catana, Cornel, McConnell, Patrick, Ohren,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 3.10 MB

english, 2013

13

Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors

Poondra, Rajamohan R., Nallamelli, Ratnam V., Meda, Chandana Lakshmi Teja, Srinivas, B.N.V., Grover, Anushka, Muttabathula, Jyotsna, Voleti, Sreedhara R., Sridhar, Balasubramanian, Pal, Manojit, Parsa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 5.05 MB

english, 2013

14

Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4–beta1 and alpha4–beta7 receptor antagonists

Sidduri, Achyutharao, Tilley, Jefferson W., Lou, Jianping, Tare, Nadine, Cavallo, Gary, Frank, Karl, Pamidimukkala, Anjula, Choi, Duk Soon, Gerber, Louise, Railkar, Aruna, Renzetti, Louis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.30 MB

english, 2013

15

A novel two-step QSAR modeling work flow to predict selectivity and activity of HDAC inhibitors

Zhao, Lingling, Xiang, Yuhong, Song, Jinglin, Zhang, Zhuoyong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 434 KB

english, 2013

16

Inhibitors of the Yersinia protein tyrosine phosphatase through high throughput and virtual screening approaches

Hu, Xin, Vujanac, Milos, Southall, Noel, Erec Stebbins, C.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.79 MB

english, 2013

17

Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors

Ting, Pauline C., Lee, Joe F., Zorn, Nicolas, Kim, Hyunjin M., Aslanian, Robert G., Lin, Mingxiang, Smith, Michelle, Walker, Scott S., Cook, John, Van Heek, Margaret, Lachowicz, Jean

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 3.25 MB

english, 2013

18

Synthesis, biological evaluation, 3D-QSAR studies of novel aryl-2H-pyrazole derivatives as telomerase inhibitors

Luo, Yin, Zhang, Shuai, Qiu, Ke-Ming, Liu, Zhi-Jun, Yang, Yu-Shun, Fu, Jie, Zhong, Wei-Qing, Zhu, Hai-Liang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 675 KB

english, 2013

19

Chemical constituents from the fruit of Gardenia jasminoides and their inhibitory effects on nitric oxide production

Peng, Kaifeng, Yang, Liguo, Zhao, Shizhe, Chen, Lixia, Zhao, Feng, Qiu, Feng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 267 KB

english, 2013

20

A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma

Long, Daniel D., Frieman, Bryan, Hegde, Sharath S., Hill, Craig M., Jiang, Lan, Kintz, Samuel, Marquess, Daniel G., Purkey, Hans, Shaw, Jeng-Pyng, Steinfeld, Tod, Wilson, Michael S., Wrench, Kevin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 642 KB

english, 2013

21

Tryptanthrin derivatives as Toxoplasma gondii inhibitors—structure–activity-relationship of the 6-position

Krivogorsky, Bogdana, Nelson, Amber C., Douglas, Kelsi A., Grundt, Peter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 366 KB

english, 2013

22

Pentacyclic hemiacetal sterol with antifouling and cytotoxic activities from the soft coral Nephthea sp.

Zhang, Jun, Li, Liang-Chun, Wang, Kai-Ling, Liao, Xiao-Jian, Deng, Zhou, Xu, Shi-Hai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 341 KB

english, 2013

23

Radiolytic transformation of rotenone with potential anti-adipogenic activity

Park, Chul-Hong, Chung, Byung Yeoup, Lee, Seung Sik, Bai, Hyoung-Woo, Cho, Jae Young, Jo, Cheorun, Kim, Tae Hoon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 350 KB

english, 2013

24

Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: Use of a conformation-based hypothesis to facilitate compound design

Walker, Daniel P., Arhancet, Graciela B., Lu, Hwang-Fun, Heasley, Steven E., Metz, Sue, Kablaoui, Natasha M., Franco, Francisco M., Hanau, Cathleen E., Scholten, Jeffrey A., Springer, John R., Fobian,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.00 MB

english, 2013

25

Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold

Valdenaire, Anja, Pothier, Julien, Renneberg, Dorte, Riederer, Markus A., Peter, Oliver, Leroy, Xavier, Gnerre, Carmela, Fretz, Heinz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 899 KB

english, 2013

26

Pyrazole-based arylalkyne Cathepsin S inhibitors. Part III: Modification of P4 region

Wiener, John J.M., Wickboldt, Alvah Tyson, Nguyen, Steven, Sun, Siquan, Rynberg, Raymond, Rizzolio, Michele, Karlsson, Lars, Edwards, James P., Grice, Cheryl A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.56 MB

english, 2013

27

Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors

Jin, Meizhong, Wang, Jing, Kleinberg, Andrew, Kadalbajoo, Mridula, Siu, Kam W., Cooke, Andrew, Bittner, Mark A., Yao, Yan, Thelemann, April, Ji, Qunsheng, Bhagwat, Shripad, Mulvihill, Kristen M., Rech

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.17 MB

english, 2013

28

Synthesis and biological evaluation of substituted 2-benzoylpyridine thiosemicarbazones: Novel structure–activity relationships underpinning their anti-proliferative and chelation efficacy

Lukmantara, Adeline Y., Kalinowski, Danuta S., Kumar, Naresh, Richardson, Des R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 738 KB

english, 2013

29

Synthesis and characterization of oligonucleotide conjugates bearing electroactive labels

Moreau, Julie, Dendane, Nabil, Schöllhorn, Bernd, Spinelli, Nicolas, Fave, Claire, Defrancq, Eric

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 441 KB

english, 2013

30

Mitochondrial dysfunction contributes to the cytotoxicity of some 3,5-bis(benzylidene)-4-piperidone derivatives in colon HCT-116 cells

Helal, Muath, Das, Umashankar, Bandy, Brian, Islam, Azharul, Nazarali, Adil J., Dimmock, Jonathan R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 415 KB

english, 2013

31

Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Li, Fei, Park, Yunjeong, Hah, Jung-Mi, Ryu, Jae-Sang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.23 MB

english, 2013

32

Indenoindolone derivatives as topoisomerase II–inhibiting anticancer agents

Kashyap, Maneesh, Kandekar, Somnath, Baviskar, Ashish T., Das, Dipon, Preet, Ranjan, Mohapatra, Purusottam, Satapathy, Shakti Ranjan, Siddharth, Sumit, Guchhait, Sankar K., Kundu, Chanakya N., Banerje

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 747 KB

english, 2013

33

Enhancing nicotine vaccine immunogenicity with liposomes

Lockner, Jonathan W., Ho, Sam On, McCague, Karen C., Chiang, Su Ming, Do, Thai Q., Fujii, Gary, Janda, Kim D.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 427 KB

english, 2013

34

Novel fluorescent risedronates: Synthesis, photodynamic inactivation and imaging of Bacillus subtilis

Zhou, Li-Sheng, Yang, Ke-Wu, Feng, Lei, Xiao, Jian-Min, Liu, Cheng-Cheng, Zhang, Yi-Lin, Crowder, Michael W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 896 KB

english, 2013

35

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 30 KB

english, 2013

36

A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones

Ferrie, John J., Gruskos, Jessica J., Goldwaser, Ari L., Decker, Megan E., Guarracino, Danielle A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 760 KB

english, 2013

37

Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual acting α4β1 and α4β7 receptor antagonists

Tilley, Jefferson W., Sidduri, Achyutharao, Lou, Jianping, Kaplan, Gerry, Tare, Nadine, Cavallo, Gary, Frank, Karl, Pamidimukkala, Anjula, Choi, Duk Soon, Gerber, Louise, Railkar, Aruna, Renzetti, Lou

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.24 MB

english, 2013

38

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.60 MB

english, 2013

39

Specific chlorination of isoquinolines by a fungal flavin-dependent halogenase

Zeng, Jia, Lytle, Anna K., Gage, David, Johnson, Sean J., Zhan, Jixun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 451 KB

english, 2013

40

The interaction of cisplatin with a human telomeric DNA sequence containing seventeen tandem repeats

Nguyen, Hanh T.Q., Galea, Anne M., Murray, Vincent

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 587 KB

english, 2013

41

Corrigendum to “Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist” [Bioorg. Med. Chem. Lett. 21 (2011) 5568–5572]

Sime, Mairi, Allan, Amanda C., Chapman, Paul, Fieldhouse, Charlotte, Giblin, Gerard M.P., Healy, Mark P., Lambert, Millard H., Leesnitzer, Lisa M., Lewis, Ann, Merrihew, Raymond V., Rutter, Richard A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 117 KB

english, 2013

42

Chemical screening of an inhibitor for gibberellin receptors based on a yeast two-hybrid system

Yoon, Jung-Min, Nakajima, Masatoshi, Mashiguchi, Kiyoshi, Park, Seung-Hyun, Otani, Masato, Asami, Tadao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 374 KB

english, 2013

43

Novel diaryl ureas with efficacy in a mouse model of malaria

Anderson, John W., Sarantakis, Dimitri, Terpinski, Jacek, Santha Kumar, T.R., Tsai, Han-Chun, Kuo, Mack, Ager, Arba L., Jacobs, William R., Schiehser, Guy A., Ekins, Sean, Sacchettini, James C., Jacob

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 422 KB

english, 2013

44

Novel berberine triazoles: Synthesis, antimicrobial evaluation and competitive interactions with metal ions to Human Serum Albumin

Zhang, Shao-Lin, Chang, Juan-Juan, Damu, Guri L.V., Fang, Bo, Zhou, Xiang-Dong, Geng, Rong-Xia, Zhou, Cheng-He

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 407 KB

english, 2013

45

The extremo-α-carbonic anhydrase (CA) from Sulfurihydrogenibium azorense, the fastest CA known, is highly activated by amino acids and amines

Akdemir, Atilla, Vullo, Daniela, Luca, Viviana De, Scozzafava, Andrea, Carginale, Vincenzo, Rossi, Mosè, Supuran, Claudiu T., Capasso, Clemente

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 325 KB

english, 2013

46

Synthesis of 2,6-difluoro-N-(3-[11C]methoxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide as a new potential PET agent for imaging of B-RafV600E in cancers

Wang, Min, Gao, Mingzhang, Miller, Kathy D., Zheng, Qi-Huang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 443 KB

english, 2013