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Structural correlates of antifungal and cytotoxic activity of brefeldin A: the importance of a rigid planar lactone ring.

作者信息

Crabbe M J, Betina V

机构信息

Department of Microbiology, University of Reading, Whiteknights, United Kingdom.

出版信息

Folia Microbiol (Praha). 1994;39(5):445-8. doi: 10.1007/BF02814454.

DOI:10.1007/BF02814454
PMID:7729778
Abstract

Molecular modelling of brefeldin A and its derivatives shows that the presence of a rigid and planar lactone ring conformation is necessary for cytotoxic and anti-fungal activity. Cytotoxic compounds had lactone ring torsion angles of -28.77 +/- 6.13 degrees, while non-cytotoxic compounds had torsion angles of -88.25 +/- 14.6 degrees.

摘要

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Molecular modelling of HIV-1 reverse transcriptase inhibitors.HIV-1逆转录酶抑制剂的分子建模
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Biological effects of the antibiotic brefeldin A (decumbin, cyanein, ascotoxin, synergisidin): a retrospective.
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7
Brefeldin A inhibits protein synthesis in cultured cells.布雷菲德菌素A抑制培养细胞中的蛋白质合成。
FEBS Lett. 1992 Dec 21;314(3):371-4. doi: 10.1016/0014-5793(92)81508-j.
8
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Pharmazie. 1992 Aug;47(8):582-4.