环戊烯-[g]环化异茚三酮模型的合成与抗肿瘤活性。

IF 1.8 4区生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2024-02-29 Print Date: 2024-01-29 DOI:10.1515/znc-2023-0119

Mustafa M El-Abadelah, Ahmad H Abdullah, Jalal A Zahra, Salim S Sabri, Sanaa K Bardaweel, Mutasem O Taha

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引用次数: 0

摘要

我们制备了一组环戊烯-[g]环化异茚三酮（5a-g），并测试了它们对 MCF-7 和 HL60 细胞的体外抗增殖活性。其中，N-1-甲基-5'-硝基衍生物（5g）对 HL60 细胞的活性最高（IC50 = 67 nM），是最有效的 Flt3 抑制剂。化合物 5d-g 对 MCF-7 具有中等活性（IC50 = 50-80 μM）。

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Synthesis and antitumor activity of model cyclopentene-[g]annelated isoindigos.

A set of cyclopenten-[g]annelated isoindigos (5a-g) has been prepared and tested for their in vitro antiproliferative activities against MCF-7 and HL60 cells. Among, the N-1-methyl-5'-nitro derivative (5g) displayed the highest activity against HL60 cells (IC₅₀ = 67 nM) and acted as the most potent Flt3 inhibitor. Compounds 5d-g exhibited moderate activity against MCF-7 (IC₅₀ = 50-80 μM).

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来源期刊

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences 生物-生化与分子生物学

CiteScore

4.10

自引率

5.00%

发文量

期刊介绍： A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) is an international scientific journal and a community resource for the emerging field of natural and natural-like products. The journal publishes original research on the isolation (including structure elucidation), bio-chemical synthesis and bioactivities of natural products, their biochemistry, pharmacology, biotechnology, and their biological activity and innovative developed computational methods for predicting the structure and/or function of natural products. A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) welcomes research papers in fields on the chemistry-biology boundary which address scientific ideas and approaches to generate and understand natural compounds on a molecular level and/or use them to stimulate and manipulate biological processes.