Document Detail

Ultrasound-promoted synthesis and immunosuppressive activity of novel quinazoline derivatives.
MedLine Citation:
PMID:  22890961     Owner:  NLM     Status:  Publisher    
An environmentally friendly and mild Bischler cyclization was developed to access quinazolines with diverse substitution. Based on this method, a library of 53 quinazoline derivatives was prepared and tested in vitro for cytotoxicity and inhibition on T-cell and B-cell proliferation. Compounds 6b, 7b, 17b, 33, and 35 showed higher inhibitory activity on both T-cell and B-cell proliferations, with IC(50) values of 6.16, 6.30, 5.43, 2.54, and 9.80 μM on T-cell, respectively. All the tested compounds showed no obvious cytotoxicity at 10 μM concentration. The preliminary structure-activity relationship was concluded revealing that 4-position is the key modification site for potent quinazoline immunosuppressive agent.
Lei Zhang; Zhe Gao; Chen Peng; Zheng-Yang Bin; Dan Zhao; Jing Wu; Qiang Xu; Jian-Xin Li
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-8-14
Journal Detail:
Title:  Molecular diversity     Volume:  -     ISSN:  1573-501X     ISO Abbreviation:  Mol. Divers.     Publication Date:  2012 Aug 
Date Detail:
Created Date:  2012-8-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9516534     Medline TA:  Mol Divers     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
State Key lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, 210093, People's Republic of China.
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