Biological Evaluation of 3-Aminoisoquinolin-1(2H)-one Derivatives as Potential Anticancer Agents Authors Lyudmyla Potikha

IF 0.4 Q4 CHEMISTRY, ANALYTICAL French-Ukrainian Journal of Chemistry Pub Date : 2021-01-01 DOI:10.17721/fujcv9i2p52-63
L. Potikha, V. Brovarets, V. Zhirnov
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Abstract

Anticancer activity of a series of 3-(hetaryl/aryl)amino substituted isoquinolin-1(2H)-ones has been studied within the international scientific program “NCI-60 Human Tumor Cell Lines Screen”. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, epithelial cancer, leukemia, and melanoma. The most effective compounds were those with thiazolyl or pyrazolyl substituent at 3-amino group and had no substituents at C(4) of the isoquinoline cycle. We identified a new lead compound, 3-(1,3-thiazol-2-ylamino)isoquinolin-1(2H)-one 12, which effectively prevents tumor cell growth (average lg GI50 = -5.18, lg TGI = -4.1, lg LC50 > -4.0) with good selectivity.
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3-氨基异喹啉-1(2H)- 1衍生物作为潜在抗癌药物的生物学评价
在国际科学项目“NCI-60人类肿瘤细胞系筛选”中,研究了一系列3-(乙基/芳基)氨基取代异喹啉-1(2H)-的抗癌活性。对肺、肾、中枢神经系统、卵巢、前列腺、乳腺癌、上皮癌、白血病和黑色素瘤等60种细胞系进行体外筛选。在异喹啉环的C(4)上没有取代基,而在3-氨基上有噻唑基或吡唑基取代基的化合物是最有效的。我们发现了一个新的先导化合物,3-(1,3-噻唑-2-氨基)异喹啉-1(2H)- 1 12,它能有效地抑制肿瘤细胞的生长(平均lg GI50 = -5.18, lg TGI = -4.1, lg LC50 > -4.0),具有良好的选择性。
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来源期刊
French-Ukrainian Journal of Chemistry
French-Ukrainian Journal of Chemistry CHEMISTRY, ANALYTICAL-
自引率
0.00%
发文量
13
审稿时长
4 weeks
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