取代的希夫碱衍生物的合成、体外细胞毒性活性和光学分析。

IF 3.1 4区 化学 Q2 BIOCHEMICAL RESEARCH METHODS
Journal of Fluorescence Pub Date : 2025-06-01 Epub Date: 2024-06-24 DOI:10.1007/s10895-024-03803-9
Muhammad Saleem, Abrar Hussain, Muhammad Hanif, Hufsa Ahmad, Salah Uddin Khan, Sajjad Haider, Muhammad Rafiq, Rizwan Nasir Paracha, Sang Hyun Park
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引用次数: 0

摘要

具有读出传输功能的荧光细胞毒性化合物在化疗中至关重要。这些治疗策略日益增长的需求要求新型杂环分子具有更好的选择性和荧光标记潜力。在此背景下,我们合成、表征并评估了一系列 9 种异atin 希夫碱衍生物 4a-i,包括紫外可见光、荧光、热和生物分析,以探索结构对其生物特性的影响。类似物 4d 对海拉细胞表现出最大的细胞毒性活性,50 µM 和 150 µM 浓度下的抑制率分别为 83% 和 100%;4c 表现出最小的细胞毒性活性,50 µM 和 150 µM 浓度下的抑制率分别为 19% 和 22%。同时,研究发现 4g 对 Vero 细胞的抑制潜力最大,在 50 µM 浓度下的抑制百分比为 83%。总体 SAR 研究表明,对氟取代的靛红分子具有明显的抑制百分比,而对溴取代的靛红衍生物活性最低。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis, Invitro Cytotoxic Activity and Optical Analysis of Substituted Schiff Base Derivatives.

Synthesis, Invitro Cytotoxic Activity and Optical Analysis of Substituted Schiff Base Derivatives.

Fluorescent cytotoxic compounds with readout delivery are crucial in chemotherapy. The growing demands of these treatment strategies require the novel heterocyclic molecules with better selectivity alongside fluorescence marker potential. In this context, a series of nine isatin Schiff base derivatives 4a-i were synthesized, characterized and evaluated for UV-visible, fluorescence, thermal and bioanalysis in order to explore the effect of structure on their bioprofiles. The analogue 4d exhibited maximum cytotoxic activity on Hella cells with percentage inhibition of 83% at 50 µM and 100% at 150 µM concentrations while 4c showed minimum cytotoxic activity with the value of 19% at 50 µM and 22% at 150 µM concentrations. Meanwhile, 4g was found to exhibit maximum inhibition potential towards Vero Cells with the percentage inhibition values of 83 at 50 µM concentration. The overall SAR study showed that the para-fluoro-substituted isatin moieties exhibited the appreciable percentage inhibition while the least activity was delivered by the isatin derivatives with para-bromo substitution.

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来源期刊
Journal of Fluorescence
Journal of Fluorescence 化学-分析化学
CiteScore
4.60
自引率
7.40%
发文量
203
审稿时长
5.4 months
期刊介绍: Journal of Fluorescence is an international forum for the publication of peer-reviewed original articles that advance the practice of this established spectroscopic technique. Topics covered include advances in theory/and or data analysis, studies of the photophysics of aromatic molecules, solvent, and environmental effects, development of stationary or time-resolved measurements, advances in fluorescence microscopy, imaging, photobleaching/recovery measurements, and/or phosphorescence for studies of cell biology, chemical biology and the advanced uses of fluorescence in flow cytometry/analysis, immunology, high throughput screening/drug discovery, DNA sequencing/arrays, genomics and proteomics. Typical applications might include studies of macromolecular dynamics and conformation, intracellular chemistry, and gene expression. The journal also publishes papers that describe the synthesis and characterization of new fluorophores, particularly those displaying unique sensitivities and/or optical properties. In addition to original articles, the Journal also publishes reviews, rapid communications, short communications, letters to the editor, topical news articles, and technical and design notes.
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