Volume 123

European Journal of Medicinal Chemistry

Volume 123

1

Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase

Kantsadi, Anastassia L., Bokor, Éva, Kun, Sándor, Stravodimos, George A., Chatzileontiadou, Demetra S.M., Leonidas, Demetres D., Juhász-Tóth, Éva, Szakács, Andrea, Batta, Gyula, Docsa, Tibor, Gergely,

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.62 MB

english, 2016

2

Arylthiosemicarbazones as antileishmanial agents

Manzano, José Ignacio, Cochet, Florent, Boucherle, Benjamin, Gómez-Pérez, Verónica, Boumendjel, Ahcène, Gamarro, Francisco, Peuchmaur, Marine

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 765 KB

english, 2016

3

Synthesis, X-ray crystal structure and anti-tumor activity of calix[n]arene polyhydroxyamine derivatives

An, Lin, Han, Li-Li, Zheng, You-Guang, Peng, Xian-Na, Xue, Yun-Sheng, Gu, Xiao-Ke, Sun, Jing, Yan, Chao-Guo

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.74 MB

english, 2016

4

Synthesis, anticancer activity and photostability of novel 3-ethyl-2-mercapto-thieno[2,3-d]pyrimidin-4(3H)-ones

Mavrova, Anelia Ts, Dimov, Stefan, Yancheva, Denitsa, Rangelov, Miroslav, Wesselinova, Diana, Tsenov, Jordan A.

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.41 MB

english, 2016

5

Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives

Ruddarraju, Radhakrishnam Raju, Murugulla, Adharvana Chari, Kotla, Ravindar, Chandra Babu Tirumalasetty, Muni, Wudayagiri, Rajendra, Donthabakthuni, Shobha, Maroju, Ravichandar, Baburao, K., Parasa, L

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.41 MB

english, 2016

6

Synthesis and immunopotentiating activity of novel isoxazoline functionalized coumarins

Ismail, Tabasum, Shafi, Syed, Singh, Swarn, Sidiq, Tabasum, Khajuria, Anamika, Rouf, Abdul, Yadav, Mahipal, Saikam, Varma, Singh, Parvinder Pal, Alam, Mohammad Sarwar, Islam, Nasarul, Sharma, Kalichar

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 864 KB

english, 2016

7

Pyrrolidinone and pyrrolidine derivatives: Evaluation as inhibitors of InhA and Mycobacterium tuberculosis

Matviiuk, Tetiana, Madacki, Jan, Mori, Giorgia, Orena, Beatrice Silvia, Menendez, Christophe, Kysil, Andrii, André-Barrès, Christiane, Rodriguez, Frédéric, Korduláková, Jana, Mallet-Ladeira, Sonia, Vo

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 3.27 MB

english, 2016

8

Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX

Pourabdi, Ladan, Khoobi, Mehdi, Nadri, Hamid, Moradi, Alireza, Moghadam, Farshad Homayouni, Emami, Saeed, Mojtahedi, Mohammad M., Haririan, Ismaeil, Forootanfar, Hamid, Ameri, Alieh, Foroumadi, Alirez

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 818 KB

english, 2016

9

Computer-aided identification, synthesis and evaluation of substituted thienopyrimidines as novel inhibitors of HCV replication

Bassetto, Marcella, Leyssen, Pieter, Neyts, Johan, Yerukhimovich, Mark M., Frick, David N., Brancale, Andrea

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.40 MB

english, 2016

10

Identification of new potent phthalazine derivatives with VEGFR-2 and EGFR kinase inhibitory activity

Amin, Kamilia M., Barsoum, Flora F., Awadallah, Fadi M., Mohamed, Nehal E.

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 647 KB

english, 2016

11

2,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5

Xu, Zhongliang, Guo, Jiamei, Yang, Ying, Zhang, Mengdi, Ba, Mingyu, Li, Zhenzhong, Cao, Yingli, He, Ricai, Yu, Miao, Zhou, Hua, Li, Xiaoxi, Huang, Xiaoshan, Guo, Ying, Guo, Changbin

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 593 KB

english, 2016

12

Biological importance of structurally diversified chromenes

Costa, Marta, Dias, Tatiana A., Brito, Alexandra, Proença, Fernanda

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.07 MB

english, 2016

13

FtsZ inhibition and redox modulation with one chemical scaffold: Potential use of dihydroquinolines against mycobacteria

Duggirala, Sridevi, Napoleon, John Victor, Nankar, Rakesh P., Senu Adeeba, V., Manheri, Muraleedharan K., Doble, Mukesh

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 3.92 MB

english, 2016

14

Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1

Wang, Yu, Zhang, Guogang, Hu, Gang, Bu, Yanxin, Lei, Hongrui, Zuo, Daiying, Han, Mengting, Zhai, Xin, Gong, Ping

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 921 KB

english, 2016

15

Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors

Lawson, Marie, Rodrigo, Jordi, Baratte, Blandine, Robert, Thomas, Delehouzé, Claire, Lozach, Olivier, Ruchaud, Sandrine, Bach, Stéphane, Brion, Jean-Daniel, Alami, Mouad, Hamze, Abdallah

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.78 MB

english, 2016

16

In vitro and in vivo studies of the antineoplastic activity of copper (II) compounds against human leukemia THP-1 and murine melanoma B16-F10 cell lines

Borges, Layla J.H., Bull, Érika S., Fernandes, Christiane, Horn, Adolfo, Azeredo, Nathalia F., Resende, Jackson A.L.C., Freitas, William R., Carvalho, Eulógio C.Q., Lemos, Luciana S., Jerdy, Hassan, K

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 3.52 MB

english, 2016

17

Synthesis and biofilm formation reduction of pyrazole-4-carboxamide derivatives in some Staphylococcus aureus strains

Cascioferro, Stella, Maggio, Benedetta, Raffa, Demetrio, Raimondi, Maria Valeria, Cusimano, Maria Grazia, Schillaci, Domenico, Manachini, Barbara, Plescia, Fabiana, Daidone, Giuseppe

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.30 MB

english, 2016

18

β-Ionone and its analogs as promising anticancer agents

Ansari, Mahsa, Emami, Saeed

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.06 MB

english, 2016

19

The therapeutic journey of pyridazinone

Akhtar, Wasim, Shaquiquzzaman, M., Akhter, Mymoona, Verma, Garima, Khan, Mohemmed Faraz, Alam, M. Mumtaz

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.15 MB

english, 2016

20

Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold

Liu, Chunchi, Luo, Changqun, Hao, Lijuan, Wu, Qiong, Xie, Honglei, Zhao, Shizhen, Hao, Chenzhou, Zhao, Dongmei, Cheng, Maosheng

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 726 KB

english, 2016

21

Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors

Li, Juanjuan, Li, Yang, Yang, Dan, Hu, Nan, Guo, Zhanling, Kuang, Chunxiang, Yang, Qing

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.66 MB

english, 2016

22

Bioevaluation of sixteen ADMDP stereoisomers toward alpha-galactosidase A: Development of a new pharmacological chaperone for the treatment of Fabry disease and potential enhancement of enzyme replacement therapy efficiency

Cheng, Wei-Chieh, Wang, Jen-Hon, Li, Huang-Yi, Lu, Sheng-Jhih, Hu, Jia-Ming, Yun, Wen-Yi, Chiu, Cheng-Hsin, Yang, Wen-Bin, Chien, Yin-Hsiu, Hwu, Wuh-Liang

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.16 MB

english, 2016

23

5-HT7 receptor modulators: Amino groups attached to biphenyl scaffold determine functional activity

Kim, Youngjae, Park, Hyeri, Lee, Jeongeun, Tae, Jinsung, Kim, Hak Joong, Min, Sun-Joon, Rhim, Hyewhon, Choo, Hyunah

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.21 MB

english, 2016

24

Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics

Chen, Xiao-Wen, Sun, Yuan-Yuan, Fu, Lei, Li, Jian-Qi

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.04 MB

english, 2016

25

Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors

Liu, Ju, Nie, Minhua, Wang, Yanjing, Hu, Jinxing, Zhang, Feng, Gao, Yanlin, Liu, Yajing, Gong, Ping

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.71 MB

english, 2016

26

Design and synthesis of 1,2,3-triazole-containing N-acyl zanamivir analogs as potent neuraminidase inhibitors

Das, Anindya, Adak, Avijit K., Ponnapalli, Kalyankumar, Lin, Chien-Hung, Hsu, Kai-Cheng, Yang, Jinn-Moon, Hsu, Tsu-An, Lin, Chun-Cheng

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.50 MB

english, 2016

27

Substituted conformationally restricted guanidine derivatives: Probing the α2-adrenoceptors’ binding pocket

McMullan, Michela, García-Bea, Aintzane, Miranda-Azpiazu, Patricia, Callado, Luis F., Rozas, Isabel

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.29 MB

english, 2016

28

α−N−heterocyclic thiosemicarbazone Fe(III) complex: Characterization of its antitumor activity and identification of anticancer mechanism

Gou, Yi, Wang, Jun, Chen, Shifang, Zhang, Zhan, Zhang, Yao, Zhang, Wei, Yang, Feng

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.49 MB

english, 2016

29

Chalcogen containing heterocyclic scaffolds: New hybrids with antitumoral activity

Alcolea, Verónica, Plano, Daniel, Encío, Ignacio, Palop, Juan Antonio, Sharma, Arun K., Sanmartín, Carmen

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.97 MB

english, 2016

30

Aromatic heterocyclic esters of podophyllotoxin exert anti-MDR activity in human leukemia K562/ADR cells via ROS/MAPK signaling pathways

Zhang, Lei, Zhang, Zeguo, Chen, Fan, Chen, Yongzheng, Lin, Ya, Wang, Jing

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.44 MB

english, 2016

31

Synthesis and antiproliferative mechanism of action of pyrrolo[3′,2′:6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers

Spanò, Virginia, Frasson, Ilaria, Giallombardo, Daniele, Doria, Filippo, Parrino, Barbara, Carbone, Anna, Montalbano, Alessandra, Nadai, Matteo, Diana, Patrizia, Cirrincione, Girolamo, Freccero, Mauro

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.26 MB

english, 2016

32

Selenoureido-iminosugars: A new family of multitarget drugs

Olsen, Jacob Ingemar, Plata, Gabriela B., Padrón, José M., López, Óscar, Bols, Mikael, Fernández-Bolaños, José G.

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 534 KB

english, 2016

33

Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase

Agharbaoui, Fatima E., Hoyte, Ashley C., Ferro, Stefania, Gitto, Rosaria, Buemi, Maria Rosa, Fuchs, James R., Kvaratskhelia, Mamuka, De Luca, Laura

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.36 MB

english, 2016

34

Slowing down fat digestion and absorption by an oxadiazolone inhibitor targeting selectively gastric lipolysis

Point, Vanessa, Bénarouche, Anais, Zarrillo, Julie, Guy, Alexandre, Magnez, Romain, Fonseca, Laurence, Raux, Brigitt, Leclaire, Julien, Buono, Gérard, Fotiadu, Frédéric, Durand, Thierry, Carrière, Fré

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 3.65 MB

english, 2016

35

Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study

Lamie, Phoebe F., Ali, Waleed A.M., Bazgier, Vaclav, Rárová, Lucie

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.55 MB

english, 2016

36

Design, synthesis and evaluation of novel potent angiotensin II receptor 1 antagonists

Bao, Xiaolu, Zhu, Weibo, Yuan, Weidong, Zhu, Xingbo, Yan, Yijia, Tang, Hesheng, Chen, Zhilong

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.26 MB

english, 2016

37

Synthesis and cytotoxicity of novel artemisinin derivatives containing sulfur atoms

Xu, Cang-Cang, Wu, Juan-Juan, Xu, Tao, Yao, Chun-Hua, Yu, Bo-Yang, Liu, Ji-Hua

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 459 KB

english, 2016

38

Synthesis and T-type calcium channel-blocking effects of aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamides for neuropathic pain treatment

Kim, Jung Hyun, Keum, Gyochang, Chung, Hesson, Nam, Ghilsoo

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 566 KB

english, 2016

39

Novel bis-arylalkylamines as myeloperoxidase inhibitors: Design, synthesis, and structure-activity relationship study

Aldib, Iyas, Gelbcke, Michel, Soubhye, Jalal, Prévost, Martine, Furtmüller, Paul G., Obinger, Christian, Elfving, Betina, Alard, Ibaa Chikh, Roos, Goedele, Delporte, Cédric, Berger, Gilles, Dufour, Da

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.71 MB

english, 2016

40

Inhibitory activity evaluation and mechanistic studies of tetracyclic oxindole derivatives as α-glucosidase inhibitors

Sun, Hua, Zhang, Yazhou, Ding, Weina, Zhao, Xue, Song, Xiaotong, Wang, Dong, Li, Yashan, Han, Kailin, Yang, Yang, Ma, Ying, Wang, Runling, Wang, Dong, Yu, Peng

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.38 MB

english, 2016

41

Synthesis and anti-leishmanial evaluation of 1-phenyl-2,3,4,9-tetrahydro-1H-β-carboline derivatives against Leishmania infantum

Ashok, Penta, Chander, Subhash, Tejería, Ana, García-Calvo, Laura, Balaña-Fouce, Rafael, Murugesan, Sankaranarayanan

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 791 KB

english, 2016

42

Studies on the inhibition of sphingosine-1-phosphate lyase by stabilized reaction intermediates and stereodefined azido phosphates

Sanllehí, Pol, Abad, José-Luís, Bujons, Jordi, Casas, Josefina, Delgado, Antonio

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.16 MB

english, 2016

43

Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors

Kim, Boyoung, Park, Hwanggue, Lee, Seul Ki, Park, Sung Jean, Koo, Tae-Sung, Kang, Nam Sook, Hong, Ki Bum, Choi, Sungwook

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.05 MB

english, 2016

44

X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors

Catalano, Alessia, Luciani, Rosaria, Carocci, Alessia, Cortesi, Debora, Pozzi, Cecilia, Borsari, Chiara, Ferrari, Stefania, Mangani, Stefano

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.15 MB

english, 2016

45

Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity

Papadopoulou, Maria V., Bloomer, William D., Rosenzweig, Howard S., Wilkinson, Shane R., Szular, Joanna, Kaiser, Marcel

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.28 MB

english, 2016

46

Editorial board

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 56 KB

english, 2016

47

Graphical contents list

Journal:

European Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 4.60 MB

english, 2016

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