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伊马替尼类似物基于片段的特权设计、合成及体外抗肿瘤活性

Privileged fragment-based design, synthesis and in vitro antitumor activity of imatinib analogues.

作者信息

Jiang Hongyu, Wang Yuankun, Jiang Maokai, Yao Lei

机构信息

School of Pharmacy, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shan-dong, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Yantai University, Yantai, China.

出版信息

Turk J Chem. 2023 Feb 14;47(2):426-435. doi: 10.55730/1300-0527.3549. eCollection 2023.

DOI:10.55730/1300-0527.3549
PMID:37528931
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10388080/
Abstract

Based on the privileged fragment-based drug design strategy, a series of imatinib analogues bearing the moiety of 3-(2-amino-2-oxoacetyl)-1H-indole were designed and synthesized, and the in vitro antitumor activity of these compounds was detected by MTT method using K562 (human myeloid leukemia) and K562R (imatinib-resistant chronic myeloid leukemia) cell lines. Molecular docking was used to preliminarily explain the possible binding modes. The most potent compound exhibited better antitumor activity than those of imatinib against K562 and K562R cancer cells with IC values of 0.8 μM and 0.7 μM.

摘要

基于特权片段药物设计策略，设计并合成了一系列带有3-(2-氨基-2-氧代乙酰基)-1H-吲哚部分的伊马替尼类似物，并使用K562（人髓性白血病）和K562R（伊马替尼耐药慢性髓性白血病）细胞系通过MTT法检测了这些化合物的体外抗肿瘤活性。采用分子对接初步解释其可能的结合模式。最有效的化合物对K562和K562R癌细胞表现出比伊马替尼更好的抗肿瘤活性，IC值分别为0.8 μM和0.7 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/a3694f643241/turkjchem-47-2-426f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/69ba0efd4d91/turkjchem-47-2-426f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/777fb7c7bf85/turkjchem-47-2-426f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/5e065349d0af/turkjchem-47-2-426f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/a3694f643241/turkjchem-47-2-426f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/69ba0efd4d91/turkjchem-47-2-426f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/777fb7c7bf85/turkjchem-47-2-426f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/5e065349d0af/turkjchem-47-2-426f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d1d/10388080/a3694f643241/turkjchem-47-2-426f4.jpg

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