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

被引：41

作者：

Belal, Amany ^{[1
,2
]}

Abdelgawad, Mohamed A. ^{[3
,4
]}

机构：

[1] Beni Suef Univ, Fac Pharm, Dept Med Chem, Bani Suwayf 62514, Egypt

[2] Taif Univ, Dept Pharmaceut Chem, Coll Pharm, At Taif 21974, Saudi Arabia

[3] Beni Suef Univ, Dept Organ Pharmaceut Chem, Bani Suwayf 62514, Egypt

[4] Aljouf Univ, Coll Pharm, Dept Pharmaceut Chem, Sakaka Aljouf 2014, Saudi Arabia

来源：

RESEARCH ON CHEMICAL INTERMEDIATES | 2017年 / 43卷 / 07期

关键词：

Pyrazole; Benzothiazole; Benzoxazole; COX inhibitors; Anticancer; CYCLOOXYGENASE-2; INHIBITOR; ENDOTHELIAL-CELLS; CANCER CELLS; BENZOXAZOLE DERIVATIVES; BIOLOGICAL EVALUATION; GENE-EXPRESSION; CELECOXIB; AGENTS; INDUCTION; DISCOVERY;

D O I：

10.1007/s11164-016-2851-x

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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 A mu M 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.

引用

页码：3859 / 3872

页数：14

共 32 条

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