- Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles
[作者：Chidananda, N; Poojary, B; Sumangala, V; Kumari, NS; Shetty, P; Arulmoli, T,期刊：European Journal of Medicinal Chemistry, 页码：124-136 , 文章类型： Article，,卷期：2012年51-1]
- Two new series of compounds namely, 3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadizoles (5a-j) and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadizoles (7a-j) were prepared. In continuation of a pr...
- Synthesis and biological evaluation of novel bifendate derivatives bearing 6, 7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors
[作者：Gu, XK; Ren, ZG; Tang, XB; Peng, H; Zhao, Q; Lai, YS; Peng, SX; Zhang, YH,期刊：European Journal of Medicinal Chemistry, 页码：137-144 , 文章类型： Article，,卷期：2012年51-1]
- Overexpression of P-glycoprotein (P-gp) is one of the major problems in successful treatment of cancers. To find new P-gp inhibitors, a series of bifendate (DDB) derivatives bearing dibenzo[c,e]azepine scaffold were synt...
- Thieno[2,3-d]pyrimidinedione derivatives as antibacterial agents
[作者：Dewal, MB; Wani, AS; Vidaillac, C; Oupicky, D; Rybak, MJ; Firestine, SM,期刊：European Journal of Medicinal Chemistry, 页码：145-153 , 文章类型： Article，,卷期：2012年51-1]
- Several thieno[2,3-d]pyrimidinediones have been synthesized and examined for antibacterial activity against a range of Gram-positive and Gram-negative pathogens. Two compounds displayed potent activity (2-16 mg/L) agains...
- Antifungal peptides at membrane interaction
[作者：Di Marino, S; Scrima, M; Grimaldi, M; D'Errico, G; Vitiello, G; Sanguinetti, M; De Rosa, M; Soriente, A; Novellino, E; D'Ursi, AM,期刊：European Journal of Medicinal Chemistry, 页码：154-162 , 文章类型： Article，,卷期：2012年51-1]
- Many drugs are available for the treatment of systemic or superficial mycoses, but only a limited number of them are effective antifungal drugs, devoid of toxic and undesirable side effects. Furthermore, resistance devel...
- Novel isoxazole polycyclic aromatic hydrocarbons as DNA-intercalating agents
[作者：Rescifina, A; Varrica, MG; Carnovale, C; Romeo, G; Chiacchio, U,期刊：European Journal of Medicinal Chemistry, 页码：163-173 , 文章类型： Article，,卷期：2012年51-1]
- The third generation of isoxazole polycyclic aromatic hydrocarbons, acting as DNA-intercalator agents and possessing the binding constants in the range 10(4)-10(5) M(-1), in order to easily diffuse targeting remotely imp...
- Novel glycolipid TLR2 ligands of the type Pam(2)Cys-alpha-Gal: Synthesis and biological properties
[作者：Thomann, JS; Monneaux, F; Creusat, G; Spanedda, MV; Heurtault, B; Habermacher, C; Schuber, F; Bourel-Bonnet, L; Frisch, B,期刊：European Journal of Medicinal Chemistry, 页码：174-183 , 文章类型： Article，,卷期：2012年51-1]
- A more complete understanding of the mechanism of action of TLR agonists has fueled the investigation of new synthetic immunoadjuvants. In this context, we designed and synthesized glycolipids of the type Pam(2)Cys-alpha...
- Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists
[作者：Wijtmans, M; Maussang, D; Sirci, F; Scholten, DJ; Canals, M; Mujic-Delic, A; Chong, M; Chatalic, KLS; Custers, H; Janssen, E; de Graaf, C; Smit, MJ; de Esch, IJP; Leurs, R,期刊：European Journal of Medicinal Chemistry, 页码：184-192 , 文章类型： Article，,卷期：2012年51-1]
- The chemokine receptor CXCR7 is an atypical G protein-coupled receptor as it preferentially signals through the beta-arrestin pathway rather than through G proteins. CXCR7 is thought to be of importance in cancer and the...
- Dimeric 3,5-bis(benzylidene)-4-piperidones: A novel cluster of tumour-selective cytotoxins possessing multidrug-resistant properties
[作者：Das, S; Das, U; Sakagami, H; Umemura, N; Iwamoto, S; Matsuta, T; Kawase, M; Molnar, J; Serly, J; Gorecki, DKJ; Dimmock, JR,期刊：European Journal of Medicinal Chemistry, 页码：193-199 , 文章类型： Article，,卷期：2012年51-1]
- A series of bis[3,5-bis(benzylidene)-4-oxo-1-piperidinyl]amides 1 display potent cytotoxic properties towards a wide range of tumours. A number of the CC(50) and IC(50) values are in the range of 10(-8) M. Specifically, ...
- Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs
[作者：Guan, YY; Zheng, D; Yan, Z; Wang, N; Lei, PS,期刊：European Journal of Medicinal Chemistry, 页码：200-205 , 文章类型： Article，,卷期：2012年51-1]
- Four 5,6-dihydro-17-hydroxy icogenin analogs were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay. Compound 22 (IC(50) = 3.38-8.30 mu M) and compound 23 (IC(50) = 1.90-...
- Synthesis of new troglitazone derivatives: Anti-proliferative activity in breast cancer cell lines and preliminary toxicological study
[作者：Salamone, S; Colin, C; Grillier-Vuissoz, I; Kuntz, S; Mazerbourg, S; Flament, S; Martin, H; Richert, L; Chapleur, Y; Boisbrun, M,期刊：European Journal of Medicinal Chemistry, 页码：206-215 , 文章类型： Article，,卷期：2012年51-1]
- Breast cancer is the most prevalent cancer in women. The development of resistances to therapeutic agents and the absence of targeted therapy for triple negative breast cancer motivate the search for alternative treatmen...
- Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step
[作者：Ramunno, A; Cosconati, S; Sartini, S; Maglio, V; Angiuoli, S; La Pietra, V; Di Maro, S; Giustiniano, M; La Motta, C; Da Settimo, F; Marinelli, L; Novellino, E,期刊：European Journal of Medicinal Chemistry, 页码：216-226 , 文章类型： Article，,卷期：2012年51-1]
- Aldose reductase (ALR2) is a crucial enzyme in the development of the major complications of diabetes mellitus. Very recently it has been demonstrated that the ARL2 inhibitor, fidarestat, significantly prevents inflammat...
- Novel NSAID 1-acyl-4-cycloalkyl/arylsemicarbazides and 1-acyl-5-benzyloxy/hydroxy carbamoylcarbazides as potential anticancer agents and antioxidants
[作者：Perkovic, I; Butula, I; Kralj, M; Martin-Kleiner, I; Balzarini, J; Hadjipavlou-Litina, D; Katsori, AM; Zorc, B,期刊：European Journal of Medicinal Chemistry, 页码：227-238 , 文章类型： Article，,卷期：2012年51-1]
- The novel 1-acyl-4-cycloalkyl/arylsemicarbazides (5a-y) and 1-acyl-5-benzyloxy/hydroxy carbamoylcarbazides (8a-f) derived from the nonsteroidal anti-inflammatory drugs ibuprofen, fenoprofen and reduced ketoprofen were pr...
- Inhibitory effect of novel S,N-bisphosphonates on some carcinoma cell lines, osteoarthritis, and chronic inflammation
[作者：Kamel, AA; Geronikaki, A; Abdou, WM,期刊：European Journal of Medicinal Chemistry, 页码：239-249 , 文章类型： Article，,卷期：2012年51-1]
- A new series of S,N-bisphosphonate derivatives was synthesized and evaluated as antitumor agents against breast-, cervix-, liver, and colon cancer diseases. Antiarthritic and antichronic inflammatory properties of the ne...
- Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents
[作者：Wang, ZW; Wu, M; Wang, Y; Li, Z; Wang, L; Han, GF; Chen, FZ; Liu, YX; Wang, KL; Zhang, A; Meng, LH; Wang, QM,期刊：European Journal of Medicinal Chemistry, 页码：250-258 , 文章类型： Article，,卷期：2012年51-1]
- A series of phenanthroindolizidine and phenanthroquinolizidine alkaloids and their 14-amino-derivatives (1-44) were prepared and systematically evaluated for their anti-tumor activities against A549 and HL60 cell lines. ...
- Design of [(2-pyrimidinylthio)acetyl]benzenesulfonamides as inhibitors of human carbonic anhydrases
[作者：Capkauskaite, E; Zubriene, A; Baranauskiene, L; Tamulaitiene, G; Manakova, E; Kairys, V; Grazulis, S; Tumkevicius, S; Matulis, D,期刊：European Journal of Medicinal Chemistry, 页码：259-270 , 文章类型： Article，,卷期：2012年51-1]
- A series of [(2-pyrimidinylthio)acetyl]benzenesulfonamides were designed and synthesized. Their binding affinities as inhibitors of several recombinant human carbonic anhydrase (CA) isozymes were determined by isothermal...
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