- Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model
[作者:Redondo, M; Zarruk, JG; Ceballos, P; Perez, DI; Perez, C; Perez-Castillo, A; Moro, MA; Brea, J; Val, C; Cadavid, MI; Loza, MI; Campillo, NE; Martinez, A; Gil, C,期刊:European Journal of Medicinal Chemistry, 页码:175-185 , 文章类型: Article,,卷期:2012年47-1]
- A simple and efficient synthetic method for the preparation of quinazoline type phosphodiesterase 7 (PDE7) inhibitors, based on microwave irradiation, has been developed. The use of this methodology improved yields and r...
- Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates
[作者:Figueiredo, R; Ramos, DF; Moiteiro, C; Medeiros, MA; Curto, MJM; de Menezes, JC; Pando, RH; Silva, PEA; Costa, MD,期刊:European Journal of Medicinal Chemistry, 页码:186-193 , 文章类型: Article,,卷期:2012年47-1]
- This paper reports the susceptibility profile to rifabutin (RFB) 1 and six recently synthesized RFB analogs 3-8, of either rifampicin (RFP) susceptible Mycobacterium tuberculosis and resistant clinical isolates from two ...
- Novel octahedral Pt(IV) complex with di-n-propyl-(S,S)-ethylenediamine-N,N '-di-2-(3-cyclohexyl)propanoato ligand exerts potent immunomodulatory effects
[作者:Miljkovic, D; Poljarevic, JM; Petkovic, F; Blazevski, J; Momcilovic, M; Nikolic, I; Saksida, T; Stosic-Grujicic, S; Grguric-Sipka, S; Sabo, TJ,期刊:European Journal of Medicinal Chemistry, 页码:194-201 , 文章类型: Article,,卷期:2012年47-1]
- We have recently reported that a novel octahedral Pt(IV) complex with di-n-propyl-(S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoato ligand has a potent cytotoxic effect on glioma, melanoma and fibrosarcoma cell li...
- Synthesis and in vitro antiproliferative evaluation of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives
[作者:Ai, Y; Liang, YJ; Liu, JC; He, HW; Chen, Y; Tang, C; Yang, GZ; Fu, LW,期刊:European Journal of Medicinal Chemistry, 页码:206-213 , 文章类型: Article,,卷期:2012年47-1]
- A series of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives variously substituted at positions 2 and 3 were synthesized and evaluated for their in vitro antiproliferative activities against a panel of six human cancer ce...
- Induction of cell cycle arrest by the carbazole alkaloid Clauszoline-I from Clausena vestita D. D. Tao via inhibition of the PKC delta phosphorylation
[作者:Lin, W; Wang, Y; Lin, SS; Li, CX; Zhou, C; Wang, SG; Huang, HQ; Liu, PQ; Ye, G; Shen, XY,期刊:European Journal of Medicinal Chemistry, 页码:214-220 , 文章类型: Article,,卷期:2012年47-1]
- Sixteen carbazole alkaloids from Clausena vestita D. D. Tao were extracted, and their anti-tumor activities were evaluated. Among the extracts, Clauszoline-I exhibited an obvious growth inhibitory activity against severa...
- Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes
[作者:Fortuna, CG; Barresi, V; Bonaccorso, C; Consiglio, G; Failla, S; Trovato-Salinaro, A; Musumarra, G,期刊:European Journal of Medicinal Chemistry, 页码:221-227 , 文章类型: Article,,卷期:2012年47-1]
- Almond and VolSurf + modelling procedures allowed the structural design of new di- and mono-heteroaryl-ethylenes. The structural modifications suggested by the molecular modelling were verified by the synthesis of the de...
- Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles
[作者:Yamuna, E; Kumar, RA; Zeller, M; Prasad, KJR,期刊:European Journal of Medicinal Chemistry, 页码:228-238 , 文章类型: Article,,卷期:2012年47-1]
- A new class of heterocycles, specifically substituted pyrazolo-, isoxazolo- and pyrimidocyclohepta[b]indoles, has been prepared by condensation of substituted 7-(hydroxymethylene)-7,8,9,10-tetrahydrocyclohepta[b]indol-6(...
- Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling
[作者:Furlan, A; Colombo, F; Kover, A; Issaly, N; Tintori, C; Angeli, L; Leroux, V; Letard, S; Amat, M; Asses, Y; Maigret, B; Dubreuil, P; Botta, M; Dono, R; Bosch, J; Piccolo, O; Passarella, D; Maina, F,期刊:European Journal of Medicinal Chemistry, 页码:239-254 , 文章类型: Article,,卷期:2012年47-1]
- The Met receptor tyrosine kinase is a promising target in anticancer therapies for its role during tumor evolution and resistance to treatment. It is characterized by an unusual structural plasticity as its active site a...
- Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin
[作者:Zhao, LM; Zhang, LM; Liu, JJ; Wan, LJ; Chen, YQ; Zhang, SQ; Yan, ZW; Jiang, JH,期刊:European Journal of Medicinal Chemistry, 页码:255-260 , 文章类型: Article,,卷期:2012年47-1]
- A series of conjugates of 5-Fluorouracil (5-FU) and emodin were synthesized by coupling trimethyl emodin with N(1), N(3) dialkylated 5-FU. The 5-FU moiety contained various substituents at the N(3)-position were linked t...
- Discovery of novel selective inhibitors of Staphylococcus aureus beta-ketoacyl acyl carrier protein synthase III
[作者:Lee, JY; Jeong, KW; Shin, S; Lee, JU; Kim, Y,期刊:European Journal of Medicinal Chemistry, 页码:261-269 , 文章类型: Article,,卷期:2012年47-1]
- beta-Ketoacyl-acyl carrier protein synthase III (KAS III) is a condensing enzyme in bacterial fatty acid synthesis and a potential target while designing novel antibiotics. In our previous report, we discovered the lead ...
- Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans
[作者:Tani, N; Rahnasto-Rilla, M; Wittekindt, C; Salminen, KA; Ritvanen, A; Ollakka, R; Koskiranta, J; Raunio, H; Juvonen, RO,期刊:European Journal of Medicinal Chemistry, 页码:270-277 , 文章类型: Article,,卷期:2012年47-1]
- Because of the increasing number of immunocompromised patients and due to problems with antifungal treatment, especially with the most widely used antifungals, azoles, there is an urgent need for new, potent and safe ant...
- Sulfur and selenium derivatives of quinazoline and pyrido[2,3-d]pyrimidine: Synthesis and study of their potential cytotoxic activity in vitro
[作者:Moreno, E; Plano, D; Lamberto, I; Font, M; Encio, I; Palop, JA; Sanmartin, C,期刊:European Journal of Medicinal Chemistry, 页码:283-298 , 文章类型: Article,,卷期:2012年47-1]
- The synthesis, cytotoxic activities and selectivities of 35 derivatives related to quinazoline and pyrido [2,3-d]pyrimidine are described. The synthesized compounds were screened in vitro against four tumoral cell lines ...
- Disubstituted quinazoline derivatives as a new type of highly selective ligands for telomeric G-quadruplex DNA
[作者:Li, Z; Tan, JH; He, JH; Long, Y; Ou, TM; Li, D; Gu, LQ; Huang, ZS,期刊:European Journal of Medicinal Chemistry, 页码:299-311 , 文章类型: Article,,卷期:2012年47-1]
- A series of 2,4-disubstituted quinazoline derivatives found to be a new type of highly selective ligand to bind with telomeric G-quadruplex DNA, and their biological properties were reported for the first time. Their int...
- Synthesis and QSAR study of novel cytotoxic spiro[3H-indole-3,2 '(1 ' H)-pyrrolo[3,4-c]pyrrole]-2,3 ',5 '(1H,2 ' aH,4 ' H)-triones
[作者:Girgis, AS; Stawinski, J; Ismail, NSM; Farag, H,期刊:European Journal of Medicinal Chemistry, 页码:312-322 , 文章类型: Article,,卷期:2012年47-1]
- 1,3-Dipolar cycloaddition reaction of 1-aryl-1H-pyrrole-2,5-diones 1a-e with non-stabilized azomethine ylides, generated in situ via decarboxylative condensation of isatins 2a-c and sarcosine (3) in refluxing ethanol, af...
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