Publication: New substituted C-19-andrographolide analogues with potent cytotoxic activities
Issued Date
2012-01-01
Resource Type
ISSN
14643405
0960894X
0960894X
Other identifier(s)
2-s2.0-84655167794
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Mahidol University
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SCOPUS
Bibliographic Citation
Bioorganic and Medicinal Chemistry Letters. Vol.22, No.1 (2012), 49-52
Suggested Citation
Uthaiwan Sirion, Sakkasem Kasemsook, Kanoknetr Suksen, Pawinee Piyachaturawat, Apichart Suksamrarn, Rungnapha Saeeng New substituted C-19-andrographolide analogues with potent cytotoxic activities. Bioorganic and Medicinal Chemistry Letters. Vol.22, No.1 (2012), 49-52. doi:10.1016/j.bmcl.2011.11.085 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/13866
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Title
New substituted C-19-andrographolide analogues with potent cytotoxic activities
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Abstract
Andrographolide, the major diterpenoid lactone from Andrographis paniculata, is toxic against cancer cells. In the present study, we investigated the structure-activity relationships (SARs) of 19 andrographolide analogues which were synthesized by modification at the three hydroxyl groups. A number of the andrographolide analogues showed much higher cytotoxic activities than that of the parent compound on cancer cells including P-388, KB, COL-2, MCF-7, LU-1 and ASK cells. SAR studies of the synthetic analogues indicated that the introduction of silyl ether or triphenylmethyl ether group into C-19 of the parent compound led to increase in toxicity against the cancer cells. The 19-O-triphenylmethyl ether analogue 18 showed higher cytotoxic activity than the potent anticancer drug ellipticine, and this analogue may serve as a potential structure lead for the development of new anticancer drugs. © 2011 Elsevier Ltd. All rights reserved.