Antioxidant, α-glucosidase inhibitory and in vitro antitumor activities of coumarin-benzothiazole hybrids

被引:8
作者
Gabr, Moustafa T. [1 ,2 ]
机构
[1] Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt
[2] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA
关键词
antitumor activity; benzothiazoles; coumarins; hybridization; pharmacophore; MOLECULAR DOCKING; OXIDATIVE STRESS; DERIVATIVES; CANCER; BROMOPHENOLS; FLAVONOIDS;
D O I
10.1515/hc-2018-0101
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Coumarin-benzothiazole hybrids are antitumor agents based on their antioxidant and a-glucosidase inhibitory activities. Compounds 5a-c were selected by National Cancer Institute (NCI), USA, to be screened for antitumor activity at a single dose (10 mu m) against a panel of 60 cancer cell lines. The most active compound 5c was further screened at a five-dose level by NCI. Compound 5c displays half maximal growth inhibition (GI(50)) values of 0.24 and 0.33 mu m against central nervous system (CNS) cancer-(SNB-75) and ovarian cancer (OVCAR-4) cell lines, respectively. Compounds 5a-c were also screened for their antioxidant and alpha-glucosidase inhibitory activities.
引用
收藏
页码:243 / 247
页数:5
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