Evaluation of new naphthalimides as potential anticancer agents against breast cancer MCF-7, pancreatic cancer BxPC-3 and colon cancer HCT-15 cell lines.

Noro, J.; Maciel, J.; Duarte, D.; Olival, A.C.D.; Baptista, C.; Silva, A.C.D.; Alves, M.J.; Kong Thoo Lin, P.

Abstract

New 1,8-naphthalimido derivatives with 2,3 and 4 carbon chains bearing a number of different functionalities were synthesized and tested against a panel of breast cancer MCF-7, colon cancer HCT-15 and pancreatic cancer BxPC-3 cell lines. Generally structures with shorter alkyl chains were more active, with the one exception of the amide containing a p-nitrophenyl group. GI50 values (uM) were determined for the most active compounds. Three compounds exhibited GI50 values below 5 uM, two with MCF-7 cells, and one other with HCT-15. Compounds with different functionalities demonstrated cell line specificity: the MCF-7 cell line was more sensitive to an urea derivative (6f), the growth of HCT- 15 cells were most affected by a triazole (9d), while the BxPC-3 cell line was inhibited in a higher extend by a guanidine (4a).

Citation

NORO, J., MACIEL, J., DUARTE, D., OLIVAL, A.C.D., BAPTISTA, C., SILVA, A.C.D., ALVES, M.J. and KONG THOO LIN, P. 2015. Evaluation of new naphthalimides as potential anticancer agents against breast cancer MCF-7, pancreatic cancer BxPC-3 and colon cancer HCT-15 cell lines. Organic chemistry: current research [online], 4(3), ID 1000144. Available from: https://doi.org/10.4172/2161-0401.1000144

• Journal Article Type: Article
• Acceptance Date: Jul 13, 2015
• Online Publication Date: Jul 20, 2015
• Publication Date: Sep 30, 2015
• Deposit Date: Apr 20, 2016
• Publicly Available Date: Apr 20, 2016
• Journal: Organic chemistry: current research
• Electronic ISSN: 2161-0401
• Publisher: OMICS International
• Peer Reviewed: Peer Reviewed
• Volume: 4
• Issue: 3
• Article Number: 1000144
• DOI: https://doi.org/10.4172/2161-0401.1000144
• Keywords: Toxicity; Tetrabromide; Naphthalimide; Isocyanate; Membrane permeabilisation
• Public URL: http://hdl.handle.net/10059/1446
• Contract Date: Apr 20, 2016