New benzothiazole/benzoxazole-pyrazole hybrids with potential as COX inhibitors: design, synthesis and anticancer activity evaluation

New benzothiazole/benzoxazole-pyrazole hybrids with potential as COX inhibitors: design,... Ten new hybrids were designed and synthesized, their chemical structures were confirmed through spectral and elemental analysis. The new hybrids were screened against lung, breast and liver cancer cell lines (A549, MCF7 and Hep3B), in addition to normal fibroblast cells. Compound 13a was the most active and selective one on the lung cancer cell line (A549), its IC50 and S.I. values were 2.4 µM and 83.2, respectively. Compound 14b was active on MCF7 with the best selectivity towards this cell line. The new derivatives were screened for their inhibitory activity against COX enzymes, the obtained results revealed that compound 13a and 14b were more active inhibitors for COX-2 than celecoxib. This finding encourages us to consider COX-2 inhibitory activity as a proposed mechanism for their anticancer activity. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

New benzothiazole/benzoxazole-pyrazole hybrids with potential as COX inhibitors: design, synthesis and anticancer activity evaluation

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Publisher
Springer Journals
Copyright
Copyright © 2017 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2851-x
Publisher site
See Article on Publisher Site

Abstract

Ten new hybrids were designed and synthesized, their chemical structures were confirmed through spectral and elemental analysis. The new hybrids were screened against lung, breast and liver cancer cell lines (A549, MCF7 and Hep3B), in addition to normal fibroblast cells. Compound 13a was the most active and selective one on the lung cancer cell line (A549), its IC50 and S.I. values were 2.4 µM and 83.2, respectively. Compound 14b was active on MCF7 with the best selectivity towards this cell line. The new derivatives were screened for their inhibitory activity against COX enzymes, the obtained results revealed that compound 13a and 14b were more active inhibitors for COX-2 than celecoxib. This finding encourages us to consider COX-2 inhibitory activity as a proposed mechanism for their anticancer activity.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Jan 5, 2017

References

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