3-呋喃-2-基-2-(4-呋喃/噻吩-2-基噻唑-2-基)丙烯腈衍生物的合成及抗癌性能

Q2 Chemistry Current Chemistry Letters Pub Date : 2022-01-01 DOI:10.5267/j.ccl.2022.4.002

Yulia Matiichuk, Y. Horak, T. Chaban, I. Chaban, V. Matiychuk

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引用次数: 0

摘要

通过(4-呋喃-2-基噻唑-2-基)- 3a和(4-噻吩-2-基噻唑-2-基)- 3b乙腈与糠醛4和5-芳基呋喃醛5a-g反应得到3-呋喃-2-基-2-(4-呋喃/噻吩-2-基噻唑-2-基)丙烯腈衍生物6a-i。抗癌活性筛查是在美国国家癌症研究所(DTP, NCI, Bethesda, Maryland, USA)的发展治疗计划框架内进行的。发现(2E)-3-(2-呋喃基)-2-[4-(2-呋喃基)-1,3-噻唑-2-基]丙烯腈(6a)和2-(4-噻吩-2-基噻唑-2-基)-丙烯腈(6h)具有较低的活性，2-(4-呋喃-2-基噻唑-2-基)丙烯腈衍生物6b-g具有中等的活性。化合物6b-g对MDA-MB-468和T-47D乳腺癌细胞系敏感。在本例中观察到细胞毒性作用，其范围为GP = -38.24 - 1.28%。

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Synthesis and anticancer properties of 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives

By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 – 1.28%.

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来源期刊

Current Chemistry Letters Chemistry-Chemistry (all)

CiteScore

4.90

自引率

0.00%

发文量

审稿时长

20 weeks

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