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Molecules 2016, 21(3), 329;

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

Faculty of Applied Sciences, Ton Duc Thang University, 19 Nguyen Huu Tho St., Tan Phong Ward, Dist. 7, Ho Chi Minh City 700000, Vietnam
Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam
Faculty of Chemical Engineering, Ho Chi Minh City University of Technology, Vietnam National University, Ho Chi Minh City, 268 Ly Thuong Kiet St, Dist. 10, Ho Chi Minh City 700000, Vietnam
Authors to whom correspondence should be addressed.
Academic Editor: Julio A. Seijas Vázquez
Received: 20 January 2016 / Revised: 1 March 2016 / Accepted: 3 March 2016 / Published: 9 March 2016
(This article belongs to the Special Issue ECSOC-19)
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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. View Full-Text
Keywords: heterocyclic chalcones; cytotoxicity; rhabdomyosarcoma; LLC-PK1 cell; MTT heterocyclic chalcones; cytotoxicity; rhabdomyosarcoma; LLC-PK1 cell; MTT

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Do, T.-H.; Nguyen, D.-M.; Truong, V.-D.; Do, T.-H.-T.; Le, M.-T.; Pham, T.-Q.; Thai, K.-M.; Tran, T.-D. Synthesis and Selective Cytotoxic Activities on Rhabdomyosarcoma and Noncancerous Cells of Some Heterocyclic Chalcones. Molecules 2016, 21, 329.

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