Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors
文献类型：期刊论文
| 作者 | Firoozpour, Loghman2; Gao, Lixin3; Moghimi, Setareh2; Pasalar, Parvin4; Davoodi, Jamshid5; Wang, Ming-Wei3 ; Rezaei, Zahra1; Dadgar, Armin6; Yahyavi, Hoda2; Amanlou, Massoud1
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| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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| 出版日期 | 2020 |
| 卷号 | 35期号:1页码:1674-1684 |
| 关键词 | Caspase inhibitor Isatin sulphonamides docking studies Pharmacophore apoptosis |
| ISSN号 | 1475-6366 |
| DOI | 10.1080/14756366.2020.1809388 |
| 通讯作者 | Firoozpour, Loghman(firoozpour@gmail.com) ; Foroumadi, Alireza(aforoumadi@yahoo.com) |
| 英文摘要 | ABTRACT In this paper, a new series of isatin-sulphonamide based derivatives were designed, synthesised and evaluated as caspase inhibitors. The compounds containing 1-(pyrrolidinyl)sulphonyl and 2-(phenoxymethyl)pyrrolidin-1-yl)sulphonyl substitution at C5 position of isatin core exhibited better results compared to unsubstituted derivatives. According to the results of caspase inhibitory activity, compound20dshowed moderate inhibitory activity against caspase-3 and -7in vitrocompared to Ac-DEVD-CHO (IC50= 0.016 +/- 0.002 mu M). Among the studied compounds, some active inhibitors with IC(50s)in the range of 2.33-116.91 mu M were identified. The activity of compound20dwas rationalised by the molecular modelling studies exhibiting the additional van der Waals interaction of N-phenylacetamide substitution along with efficacious T-shaped pi-pi and pi-cation interactions. The introduction of compound20dwith good caspase inhibitory activity will help researchers to find more potent agents. |
| WOS关键词 | SELECTIVE NONPEPTIDE INHIBITORS ; APOPTOSIS ; POTENT ; DISCOVERY ; 4-ARYL-4H-CHROMENES ; PET ; ACTIVATION ; SCAFFOLD ; DESIGN ; SERIES |
| 资助项目 | National Health and Family Planning Commission of China[2012ZX09304-011] ; National Health and Family Planning Commission of China[2013ZX09401003-005] ; National Health and Family Planning Commission of China[2013ZX09507001] ; National Health and Family Planning Commission of China[2013ZX09507-002] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Thousand Talents Program in China - Iran National Science Foundation (INSF)[96011863] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000562502300001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/292483]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Firoozpour, Loghman; Foroumadi, Alireza |
| 作者单位 | 1.Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran 2.Univ Tehran Med Sci, Inst Pharmaceut Sci TIPS, Drug Design & Dev Res Ctr, Tehran, Iran 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai, Peoples R China 4.Univ Tehran Med Sci, Fac Med, Dept Biochem, Tehran, Iran 5.Univ Tehran, Inst Biochem & Biophys, Tehran, Iran 6.Kermanshah Univ Med Sci, Pharmaceut Sci Res Ctr, Kermanshah, Iran |
| 推荐引用方式 GB/T 7714 | Firoozpour, Loghman,Gao, Lixin,Moghimi, Setareh,et al. Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2020,35(1):1674-1684. |
| APA | Firoozpour, Loghman.,Gao, Lixin.,Moghimi, Setareh.,Pasalar, Parvin.,Davoodi, Jamshid.,...&Foroumadi, Alireza.(2020).Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,35(1),1674-1684. |
| MLA | Firoozpour, Loghman,et al."Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 35.1(2020):1674-1684. |
入库方式： OAI收割
来源：上海药物研究所
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