Abstract

A series of 1,2,4-triazole-schiff hybrids were synthesized and characterized by mass spectrometry, FTIR and NMR spectroscopy. The compounds were screened for anticancer activity against human breast cancer cell line (MCF-7 and T47D) and human cervical cancer cell line (HeLa). The result indicates that newly synthesized compounds exhibit cytotoxicity to all cell lines studied. In particular, MCF-7 cells were shown to be more sensitive with EC₅₀ < 50 μM/ml with the exception of compound T2. Interestingly, T6 produced more high cytotoxicity on MCF-7 cells (< 10 μM/ml), which is comparable to cisplatin EC₅₀ 13.10 μM/ml. To further investigate the mode of cell death, early and late apoptosis studies were done on MCF-7 cells. The externalization of phosphatidylserine and DNA fragmentation supports the apoptosis as the major mode of cell death induced by derivatives on MCF-7 cells.

Graphic abstract

中文翻译：

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新型1,2,4-三唑-偶氮甲碱偶联物的合成，表征和细胞毒性研究

摘要

合成了一系列1,2,4-三唑-席夫杂化物，并通过质谱，FTIR和NMR光谱进行了表征。筛选化合物对人乳腺癌细胞系（MCF-7和T47D）和人宫颈癌细胞系（HeLa）的抗癌活性。结果表明，新合成的化合物对所有研究的细胞系均显示出细胞毒性。特别是，MCF-7细胞显示出对EC ₅₀  <50μM/ ml的敏感性更高，但化合物T2除外。有趣的是，T6对MCF-7细胞产生了更高的细胞毒性（<10μM/ ml），与顺铂EC ₅₀相当13.10μM/毫升。为了进一步研究细胞死亡的方式，对MCF-7细胞进行了早期和晚期凋亡研究。磷脂酰丝氨酸的外在化和DNA片段化支持凋亡，这是MCF-7细胞衍生物诱导的细胞死亡的主要方式。

图形摘要