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.; Lin, P. Kong Thoo
P. Kong Thoo Lin
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).
|Journal Article Type||Article|
|Publication Date||Jul 20, 2015|
|Journal||Organic chemistry: current research|
|Publisher||New Publisher Required|
|Peer Reviewed||Peer Reviewed|
|Institution 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|
|Keywords||Toxicity; Tetrabromide; Naphthalimide; Isocyanate; Membrane permeabilisation|
NORO 2015 Evaluation of new naphthalimides as potential