دورية أكاديمية
(E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity
| العنوان: | (E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity |
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| المؤلفون: | Le Cong Huan, Cao Viet Phuong, Le Cong Truc, Vo Nguyen Thanh, Hai Pham-The, Le-Thi-Thu Huong, Nguyen Thi Thuan, Eun Jae Park, A Young Ji, Jong Soon Kang, Sang-Bae Han, Phuong-Thao Tran, Nguyen-Hai Nam |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 465-478 (2019) |
| بيانات النشر: | Taylor & Francis Group, 2019. |
| سنة النشر: | 2019 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | acetohydrazides, quinazolin-4(3h)-one, cytotoxicity, caspase activation, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | In our search for novel small molecules activating procaspase-3, we have designed and synthesised a series of novel acetohydrazides incorporating quinazolin-4(3H)-ones (5, 6, 7). Biological evaluation revealed eight compounds with significant cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer). The most potent compound 5t displayed cytotoxicity up to 5-fold more potent than 5-FU. Analysis of structure-activity relationships showed that the introduction of different substituents at C-6 position on the quinazolin-4(3H)-4-one moiety, such as 6-chloro or 6-methoxy potentially increased the cytotoxicity of the compounds. In term of caspase activation activity, several compounds were found to exhibit potent effects, (e.g. compounds 7 b, 5n, and 5l). Especially, compound 7 b activated caspases activity by almost 200% in comparison to that of PAC-1. Further docking simulation also revealed that this compound potentially is a potent allosteric inhibitor of procaspase-3. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1475-6366 1475-6374 14756366 |
| العلاقة: | https://doaj.org/toc/1475-6366Test; https://doaj.org/toc/1475-6374Test |
| DOI: | 10.1080/14756366.2018.1555536 |
| الوصول الحر: | https://doaj.org/article/3442a89f91194643ba8c63488686550cTest |
| رقم الانضمام: | edsdoj.3442a89f91194643ba8c63488686550c |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2018.1555536 |