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

Heterocyclic communications

article

Moustafa T. Gabr¹ 

[1] Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University;Department of Chemistry, University of Iowa

关键词: antitumor activity;    benzothiazoles;    coumarins;    hybridization;    pharmacophore;   

DOI  :  10.1515/hc-2018-0101

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

Coumarin-benzothiazole hybrids are antitumor agents based on their antioxidant and α-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 μ 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 μ 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 α-glucosidase inhibitory activities.

【 授权许可】

CC BY|CC BY-NC-ND