Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 76, Issue -, Pages 67-78Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.02.007
Keywords
Benzothiazole; Antitumor activity; Structure-activity relationships; Structure-metabolism relationship
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Funding
- National Natural Science Foundation of China [81273364, 91213303]
- National 863 Program of China [2012AA020303]
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An antitumor activity oriented benzothiazole sublibrary was constructed from a hit compound 3 via a five stepwise procedure. All target compounds were screened for their antitumor activity against 60 human cancer cell lines. Compounds 9p, 12d and 12i, showing higher potency than hit 3, were identified. Particularly, the compound 9p gave its average 50% growth inhibition (GI(50)) at 0.38 mu M. Furthermore, incubation in human liver microsome primarily proved their metabolic stability in vitro. General structure-activity and structure-metabolism relationships were both summarized, which provides information on further strategically optimization. (C) 2014 Elsevier Masson SAS. All rights reserved.
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