Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2011 Aug 1;21(15):4462-4.
doi: 10.1016/j.bmcl.2011.06.005. Epub 2011 Jun 15.

Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: an SAR study

Shashikanth Ponnala  1 , Sandeep Chaudhary, Antonio González-Sarrias, Navindra P Seeram, Wayne W Harding
Affiliations

Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: an SAR study

Shashikanth Ponnala et al. Bioorg Med Chem Lett. .

Abstract

A series of synthetic aporphine derivatives structurally related to domesticine and nantenine (ring A, N6 and ring C truncated analogs), was evaluated in MTS cytotoxicity assays against the human colon cancer cell lines, HCT-116 and Caco-2. In general, the C1 position of ring A is tolerant of alkoxy substituents as well as a benzoyl ester functionality. Other modifications evaluated resulted in a decrease in cytotoxic activity. The most potent compounds identified had IC(50) values in the range 23-38 μM, comparable to the known cytotoxic agent, etoposide.

PubMed Disclaimer

Figures

Scheme 1
Scheme 1
Synthesis of compounds 3 and 5
Scheme 2
Scheme 2
Synthesis of compound 6
See this image and copyright information in PMC

References

    1. Jemal A, Siegel R, Xu J, Ward E. CA Cancer J Clin. 2010;60:277. - PubMed
    1. Pecic S, McAnuff MA, Harding WW. J Enzyme Inhib Med Chem. 2011;26:46. - PMC - PubMed
    1. Tang H, Wei YB, Zhang C, Ning FX, Qiao W, Huang SL, Ma L, Huang ZS, Gu LQ. Eur J Med Chem. 2009;44:2523. - PubMed
    1. Adsersen A, Kjolbye A, Dall O, Jager AK. J Ethnopharmacol. 2007;113:179. - PubMed
    1. Cabedo N, Berenguer I, Figadere B, Cortes D. Curr Med Chem. 2009;16:2441. - PubMed

Publication types

LinkOut - more resources