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Design, synthesis and of antitumor activity study of coumarin derivatives bearing benzothiazole or benzene moiety
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Jun-jie MA*, Xin NI, Kun HUANG, Yu WANG
Acta Pharmaceutica Sinica | 2019, 54(3) : 514 - 521
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Acta Pharmaceutica Sinica | 2019, 54(3): 514-521
• Original Articles •
Design, synthesis and of antitumor activity study of coumarin derivatives bearing benzothiazole or benzene moiety
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Jun-jie MA*, Xin NI, Kun HUANG, Yu WANG
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  • School of Medicine, Huaqiao University, Quanzhou 362000, China
Published: 2019-03-12 doi: 10.16438/j.0513-4870.2018-1117
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Based on coumarin core structure as the procaspase-3 activator 1541 from our previous study, twelve coumarin derivatives bearing benzothiazole or benzene moiety were designed and synthesized. Target compounds were evaluated for in vitro antitumor activity against a procaspase-3 overexpressing cancer cell line (human histiocytic lymphoma cell, U937) and a procaspase-3 no-expression cancer cell line (human breast adenocarcinoma cell, MCF-7) to rule out off-target effects. The results revealed that coumarin derivatives bearing benzothiazole showed more potent inhibition activity and selectivity against procaspase-3 over-expressing cancer cell line (U937) than procaspase-3 low-sensitive cancer cell line (MCF-7). Caspase-3 activity evaluation showed that coumarin derivatives bearing benzothiazole showed remarkable caspase-3 activation activity, among them, compound 5f displayed the strongest activity with 93% degree. Flow cytometric assay revealed that compound 5f could inhibit proliferation of tumor cells by inducing apoptosis. Procaspase-3 activity assay showed that compound 5f showed strong procaspase-3 activation activity.

benzothiazole  /  coumarin  /  design  /  synthesis  /  antitumor activity
Jun-jie MA, Xin NI, Kun HUANG, Yu WANG. Design, synthesis and of antitumor activity study of coumarin derivatives bearing benzothiazole or benzene moiety[J]. Acta Pharmaceutica Sinica, 2019 , 54 (3) : 514 -521 . DOI: 10.16438/j.0513-4870.2018-1117
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doi: 10.16438/j.0513-4870.2018-1117
  • Receive Date：2018-12-14
  • Online Date：2026-01-26
  • Published：2019-03-12
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  • Received：2018-12-14
  • Revised：2019-01-21
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    School of Medicine, Huaqiao University, Quanzhou 362000, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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