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
. 2016 Mar 9;21(3):329.
doi: 10.3390/molecules21030329.

Synthesis and Selective Cytotoxic Activities on Rhabdomyosarcoma and Noncancerous Cells of Some Heterocyclic Chalcones

Tuong-Ha Do  1 , Dai-Minh Nguyen  2 , Van-Dat Truong  3 , Thi-Hong-Tuoi Do  4 , Minh-Tri Le  5 , Thanh-Quan Pham  6 , Khac-Minh Thai  7 , Thanh-Dao Tran  8
Affiliations

Synthesis and Selective Cytotoxic Activities on Rhabdomyosarcoma and Noncancerous Cells of Some Heterocyclic Chalcones

Tuong-Ha Do et al. Molecules. .

Abstract

Chemically diverse heterocyclic chalcones were prepared and evaluated for cytotoxicity, aiming to push forward potency and selectivity. They were tested against rhabdomyosarcoma (RMS) and noncancerous cell line (LLC-PK1). The influence of heteroaryl patterns on rings A and B was studied. Heterocycle functionalities on both rings, such as phenothiazine, thiophene, furan and pyridine were evaluated. Notably, the introduction of three methoxy groups at positions 3, 4, 5 on ring B appears to be critical for cytotoxicity. The best compound, with potent and selective cytotoxicity (IC50 = 12.51 μM in comparison with the value 10.84 μM of paclitaxel), contains a phenothiazine moiety on ring A and a thiophene heterocycle on ring B. Most of the potential compounds only show weak cytoxicity on the noncancerous cell line LLC-PK1.

Keywords: LLC-PK1 cell; MTT; cytotoxicity; heterocyclic chalcones; rhabdomyosarcoma.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Structure- anticancer activity relationship of chalcone compounds [30].
Scheme 1
Scheme 1
General key step for the synthesis of heterocyclic chalcones.
See this image and copyright information in PMC

References

    1. Jemal A., Siegel R., Ward E. Cancer statistics. CA Cancer J. Clin. 2008;58:71–96. doi: 10.3322/CA.2007.0010. - DOI - PubMed
    1. Twombly R. Cancer surpasses heart disease as leading cause of death for all but the very elderly. JNCI J. Natl. Cancer Inst. 2005;97:330–331. doi: 10.1093/jnci/97.5.330. - DOI - PubMed
    1. Willam H.M., Sheri L.S. Soft tissue sarcomas of childhood. Cancer Treat. Rev. 2004;30:269–280. - PubMed
    1. Keller C., Guttridge D.C. Mechanisms of impaired differentiation in rhabdomyosarcoma. FEBS J. 2013;280:4323–4334. doi: 10.1111/febs.12421. - DOI - PMC - PubMed
    1. Pappo A.S. Rhabdomyosarcoma and other soft tissue sarcomas of childhood. Curr. Opin. Oncol. 1995;7:361–366. doi: 10.1097/00001622-199507000-00012. - DOI - PubMed

Publication types

MeSH terms

LinkOut - more resources