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ContentsArchiv der Pharmazie 32009.

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Archiv der Pharmazie
Chemistry in Life Sciences
Contents
Volume 342, No. 3, March 2009
Review
Breast Cancer, Estrogen Receptor and Ligands
Zhenlin Bai and Ronald Gust*
The discovery of the estrogen receptor b and the determination of the
crystal structures of ligand-ER ligand-binding domain complexes greatly
facilitated the investigation of hormone action through the ER. Therefore,
the relationship of breast cancer, estrogen receptor and ligands is
reviewed . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 133
Full Papers
Cerulenin Analogues as Inhibitors of Efflux Pumps in
Drug-resistant Candida albicans
Florian Diwischek, Joachim Morschhuser, and Ulrike Holzgrabe*
Due to a limited number but excessive use of antimycotics, resistances
can be observed. The most important mechanism for the development
of resistance is the overexpression of efflux pumps. Thus, cerulenin was
chosen as a lead structure for the development of efflux pump inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 150
Synthesis and In-vitro Antitumor Activities of Some Mannich
Bases of 9-Alkyl-1,2,3,4-tetrahydrocarbazole-1-ones
Jing Chen, Jianshu Lou, Tao Liu, Ru Wu, Xiaowu Dong, Qiaojun He, Bo Yang, and
Yongzhou Hu*
Microtubules are recognized as an important target for anticancer therapy.
New 2-substituted aminomethyl-9-alkyl-1,2,3,4-tetrahydrocarbazole-1-ones
5a–q were synthesized and tested for their cytotoxic activity in vitro against
four human tumor cell lines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 165
i
2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Design, Synthesis, and In-vivo Pharmacological Screening
of N,3-(Substituted Diphenyl)-5-phenyl-1H-pyrazoline-1carbothioamide Derivatives
Nadeem Siddiqui*, Perwaiz Alam, and Waquar Ahsan
The search for antiepileptic agents with more selectivity and lower
toxicity is still an area of investigation. Thus, 3,5-(substituted diphenyl)4,5-dihydro-pyrazole-1-carbothioic acid phenylamides were synthesized
and tested for their anticonvulsant, antidepressant, and lipophilic
properties. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 173
Synthesis and Cytotoxicity Screening of Piperazine-1-carbodithioate Derivatives of 2-Substituted Quinazolin-4(3H)-ones
Sheng-Li Cao*, Yan-Wen Guo, Xian-Bo Wang, Mei Zhang, Yu-Ping Feng, Yu-Yang Jiang,
Yue Wang, Qian Gao, and Jian Ren
Quinazolin-4(3H)-one analogs have drawn considerable attention in the
search for antifolates and antitumor agents. Therefore, a new series of
2-substituted-quinazolin-4(3H)-one derivatives have been designed and
screened for their inhibitory activity against A-549, HCT-8, HepG2, and
K562 cell lines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 182
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