| Ultrasound-promoted synthesis and immunosuppressive activity of novel quinazoline derivatives. | |
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MedLine Citation:
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PMID: 22890961 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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Lei Zhang; Zhe Gao; Chen Peng; Zheng-Yang Bin; Dan Zhao; Jing Wu; Qiang Xu; Jian-Xin Li |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-8-14 |
Journal Detail:
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Title: Molecular diversity Volume: - ISSN: 1573-501X ISO Abbreviation: Mol. Divers. Publication Date: 2012 Aug |
Date Detail:
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Created Date: 2012-8-14 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9516534 Medline TA: Mol Divers Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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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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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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