Synthesis, molecular modeling study, preliminary antibacterial, and antitumor evaluation of N-substituted naphthalimides and their structural analogues

被引：34
|
作者：
El-Azab, Adel S. [1 ,2 ]
Alanazi, Amer M. [1 ]
Abdel-Aziz, Naglaa I. [3 ]
Al-Suwaidan, Ibrahim A. [1 ]
El-Sayed, Magda A. A. [4 ]
El-Sherbeny, Magda A. [3 ]
Abdel-Aziz, Alaa A. -M. [1 ,3 ]
机构：
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
[2] Al Azhar Univ, Dept Organ Chem, Fac Pharm, Cairo 11884, Egypt
[3] Univ Mansoura, Dept Med Chem, Fac Pharm, Mansoura 35516, Egypt
[4] Univ Mansoura, Dept Organ Pharmaceut Chem, Fac Pharm, Mansoura 35516, Egypt
来源：
MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 05期
关键词：
Naphthalimides; Cyclic imides; Synthesis; Antibacterial activity; Antitumor evaluation; Molecular modeling; Modeling; NATIONAL-CANCER-INSTITUTE; CYCLIC-IMIDES; ANTIINFLAMMATORY ACTIVITY; BIOLOGICAL EVALUATION; DRUG DISCOVERY; DNA-BINDING; INHIBITORS; DERIVATIVES; ACID; DESIGN;
D O I：
10.1007/s00044-012-0230-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Carboxylic acid imides 1-26 have been synthesized and screened for their antibacterial against gram-positive and gram-negative organisms and their antitumor activity against 60 tumor cell lines taken from nine different organs. Compounds 12, 14, and 16 were the most active and broad-spectrum antibacterial member in this study. Compound 9 showed the most cytotoxicity with a significant inhibition for renal cancer cells. 2D-QSAR study provides details on the fine relationship linking structure and activity and offers clues for structural modifications that can improve the activity. Docking study of the compounds 12, 14, and 16 into the active site of the topoisomerase II DNA gyrase enzymes revealed a similar binding mode to bound inhibitor Clorobiocin.
引用
收藏
页码：2360 / 2375
页数：16
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