期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 6, 页码 2379-2391出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.09.015
关键词
Synthesis; 2-Thieno-4(3H)-quinazolinones; Antitumor agents; Molecular modeling
资金
- King Abdulaziz City for Science and Technology [APR-23-39]
The synthesis of some new 2-thieno-4(3H)-quinazolinone derivatives and their biological evaluation as antitumor agents using the National Cancer Institute (NCI) disease oriented antitumor screen protocol are investigated. Compounds 2-(2-thienylcarbonylamino)-5-iodo-N-(4-hydroxyphenyl)-benzamide (16), 2-(2-thieno)-6-iodo-3-phenylamino-3,4-dihydro-quina-zolin-4-one (26), and 2-(2-thieno)-4-[4-sulfonamidobenzylamino]-6-iodo-quinazoline (42), with Gl(50) values of 12.7, 10.3, 16.9 mu M, respectively, proved to be the most active members in this study, as compared to the known drug 5-FU. Conformational analysis of the most active molecules using molecular modeling and QSAR techniques enabled the understanding of the pharmacophoric requirements for 2-thieno-quinzolinone derivatives as antitumor agents. These three quinazolinone analogs (16, 26, 42) could be considered as useful templates for future development to obtain more potent antitumor agents. (C) 2008 Elsevier Masson SAS. All rights reserved.
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