Benzopyrylium salts as new anticancer, antibacterial, and antioxidant agents.
Benzopyrylium salts as new anticancer, antibacterial, and antioxidant agents.
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DOI：
10.1007/s00044-020-02685-3
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发表时间：
2021-04
期刊：
影响因子：
--
通讯作者：
Golakoti NR
中科院分区：
文献类型：
--
作者：
Kar S;Akhir A;Chopra S;Ohki S;Karanam B;Golakoti NR
苯并吡啶盐是一类尚未开发的化合物，本研究首次报道了它们作为潜在的治疗剂。本文研究了几种新型苯并吡啶盐的合成及其体外抗癌、抗菌和抗氧化性能。合成了苯并吡啶盐，并通过紫外可见光谱、红外光谱、1H-NMR、13C-NMR和质谱对其进行了表征。并对苯并吡啶盐在NCI 60细胞系上的体外抗癌活性进行了测试。PS-CP-4MO对黑色素瘤MDA-MB-435细胞株的GI50 （1.78 μM）、TGI （3.47 μM）和LC50 （6.77 μM）值均最小，对黑色素瘤、结肠癌和白血病均有选择性。机制研究表明，该化合物通过诱导凋亡抑制MCF-7癌细胞，并抑制癌细胞的集落形成和伤口愈合。抑菌研究表明，部分苯并吡啶盐对金黄色葡萄球菌（ATCC 29213）具有一定的抑菌活性，其中活性最好的化合物PS-CP-5Cl的MIC为8 μg/mL。抗氧化研究表明，它们具有良好的自由基清除能力（PS-CP-5Cl活性为抗坏血酸的1.48倍）。苯并吡啶盐在硅中的利平斯基参数的满足显示了作为潜在药效团线索的巨大药物相似性。
Benzopyrylium salts are an unexplored class of compounds and as a first, this study reports them as potential therapeutic agents. In this effort we pursue the synthesis and in vitro anticancer, antibacterial and antioxidant properties of some novel benzopyrylium salts. The benzopyrylium salts were synthesized and further characterized via UV-vis, IR, 1H-NMR, 13C-NMR and mass spectrometry. The benzopyrylium salts were tested in vitro for anticancer activity across NCI 60 cell line panel. PS-CP-4MO showed the best activity against the MDA-MB-435 cell line of melanoma cancer in terms of the least GI50 (1.78 μM), TGI (3.47 μM) and LC50 (6.77 μM) values and showed selectivity against melanoma, colon cancer and leukemia. Mechanistic studies indicate that this compound inhibits MCF-7 cancer cells by inducing apoptosis and abrogates colony formation and wound healing in the cancer cells. Antibacterial studies show that some of the benzopyrylium salts are active on S. aureus (ATCC 29213) and the best active compound PS-CP-5Cl has a MIC of 8 μg/mL. Antioxidant studies indicate that they have good free radical scavenging properties (PS-CP-5Cl showed activity 1.48 times ascorbic acid). Fulfillment of the Lipinski’s parameters of the benzopyrylium salts in silico showed tremendous drug likeness as potential pharmacophore leads.
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影响因子：
--
作者：
Arora R;Schmitt D;Karanam B;Tan M;Yates C;Dean-Colomb W
通讯作者：
Dean-Colomb W
DOI：
10.1093/jnci/83.11.757
发表时间：
1991-06-05
期刊：
JOURNAL OF THE NATIONAL CANCER INSTITUTE
影响因子：
--
作者：
MONKS, A;SCUDIERO, D;BOYD, M
通讯作者：
BOYD, M
DOI：
10.1039/jr9330000430
发表时间：
1933-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY
影响因子：
--
作者：
Heilbron, IM;Heslop, RN;Irving, F
通讯作者：
Irving, F
影响因子：
4.7
作者：
Karna, Prasanthi;Gundala, Sushma R.;Aneja, Ritu
通讯作者：
Aneja, Ritu
影响因子：
2.1
作者：
SCHIELE, C;WILHELM, A;PAAL, G
通讯作者：
PAAL, G