A New Series of Indole and Azaindole Derivatives with Oxo-dihydropyridines: Synthesis, Characterization and Cytotoxicity Studies against Breast Malignant Cell Lines

Q4 Chemistry
A. Madugula, K. Jagadeesh, D.B.N. Suresh Varma, K. G. Kadiyala, S. Pedada, Rama Swamy Guttula, U. Nagababu, Gururaja Rangaiah
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引用次数: 0

Abstract

In this investigation, a novel series of indole and azaindole comprising oxo-dihydropyridine derivatives was synthesized. From their spectral (1H NMR and FTIR) as well as elemental (MS) investigations, the structures of all the synthesized 12 oxo-dihydropyridine derivatives were determined. Cytotoxicity of synthesized twelve compound was evaluated against MDA-MB-231 malignant breast cells had been assessed. Compound 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed more percent of inhibition of growth and four more derivatives showed moderate percent of inhibition of growth counter to MDA-MB-231 malignant breast cells. The derivative 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed the highest effectiveness when assessing the IC50 value against the malignant breast cell line MDA-MB-231. Each of the compounds synthesized has a druggable character and meets Lipinski’s criteria of five.
吲哚和氮杂吲哚与氧化二氢吡啶的新系列衍生物:针对乳腺恶性细胞系的合成、表征和细胞毒性研究
本研究合成了一系列新型吲哚和氮杂吲哚氧化二氢吡啶衍生物。通过光谱(1H NMR 和 FTIR)和元素(MS)分析,确定了合成的 12 种氧化二氢吡啶衍生物的结构。评估了合成的 12 种化合物对 MDA-MB-231 恶性乳腺细胞的细胞毒性。化合物 1,6-二氨基-4-(1H-吲哚-3-基)-2-氧代-1,2-二氢吡啶-3,5-二甲腈对 MDA-MB-231 恶性乳腺细胞的生长抑制率较高,另有四种衍生物对 MDA-MB-231 恶性乳腺细胞的生长抑制率中等。在评估对恶性乳腺细胞株 MDA-MB-231 的 IC50 值时,1,6-二氨基-4-(1H-吲哚-3-基)-2-氧代-1,2-二氢吡啶-3,5-二腈衍生物显示出最高的效力。合成的每个化合物都具有可药用特性,并符合利宾斯基的五项标准。
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来源期刊
Asian Journal of Chemistry
Asian Journal of Chemistry 化学-化学综合
CiteScore
0.80
自引率
0.00%
发文量
229
审稿时长
4 months
期刊介绍: Information not localized
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