Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 13, Pages 3868-3872Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.04.069
Keywords
Rosin; Dehydroabietic acid; Apoptosis; Necrosis; Caspase; Cancer
Categories
Funding
- National Natural Science Foundation of China [91213302, 20932003, 21272102]
- Key National S&T Program Major New Drug Development of the Ministry of Science and Technology [2012ZX09504001-003]
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In this Letter, the anticancer activity of novel rosin-derivatives introducing indicated side chains at position C18 of dehydroabietic acid (DHAA) was reported. Gratifyingly, all of these derivatives showed significantly cytotoxicity toward diverse human carcinoma cell lines. We found the compound 4 could induce cell membrane damage at high concentration as well as cell apoptosis at low concentration. However, compound 5, attachment of quinidine to dehydroabietic acid via thiourea bond, only induced apoptotic cell death. In addition, all these active compounds induced apoptosis mainly through mitochondrial-dependent pathway. Interestingly, compound 5 exhibited the highest anticancer activity and little toxicity to normal cells compared with the other derivatives. Therefore, 5 merits further investigation as a potential agent for future anticancer treatment. (c) 2013 Elsevier Ltd. All rights reserved.
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