20582-55-2Relevant articles and documents
Design, synthesis and biological evaluation of novel thiazole-derivatives as mitochondrial targeting inhibitors of cancer cells
Dang, Xin,Lei, Shuwen,Luo, Shuhua,Hu, Yixin,Wang, Juntao,Zhang, Dongdong,Lu, Dan,Jiang, Faqin,Fu, Lei
, (2021/06/16)
Mitochondria are pivotal energy production sources for cells to maintain necessary metabolism activities. Targeting dysfunctional mitochondrial features has been a hotspot for mitochondrial-related disease researches. Investigation with cancerous mitochondrial metabolism is a continuing concern within tumor therapy. Herein, we set out to assess the anti-cancer activities of a novel family of TPP-thiazole derivatives based on our earlier research on mitochondrial targeting agents. Specifically, we designed and synthesized a series of TPP-thiazole derivatives and revealed by the MTT assay that most synthesized compounds effectively inhibited three cancer cell lines (HeLa, PC3 and MCF-7). After structure modifications, we explored the SAR relationships and identified the most promising compound R13 (IC50 of 5.52 μM) for further investigation. In the meantime, we performed ATP production assay to assess the selected compounds inhibitory effect on HeLa cells energy production. The results displayed the test compounds significantly restrained ATP production of cancer cells. Overall, we have designed and synthesized a series of compounds which exhibited significant cytotoxicity against cancer cells and effectively inhibited mitochondrial energy production.
Method for preparing 4-methylthiazole-5-ethyl formate
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Paragraph 0008; 0018; 0022, (2017/08/29)
The invention discloses a preparation method of 4-methylthiazole-5-ethyl formate. The preparation method comprises the following steps: taking tetrahydrofuran as a solvent and formamide and phosphorus sulfide as raw materials, dissolving the phosphorus sulfide in the tetrahydrofuran firstly, dropwise adding the formamide, carrying out reaction for 1-2h, concentrating to dry, dissolving a dried product with a low-concentration sodium hydroxide solution, carrying out extraction with ethyl acetate, drying an organic layer, and filtering and concentrating to obtain thioformamide; and taking absolute ethyl alcohol as a solvent and the thioformamide and 2-chloracetyl acetidin as raw materials, carrying out reflux reaction, concentrating a reactant to dry, dissolving the dried reactant with water, extracting with the ethyl acetate, drying an organic layer, filtering, concentrating and carrying out rectification under vacuum to obtain the 4-methylthiazole-5-ethyl formate. The preparation method provided by the invention is low in cost and convenient to operate.
5 - thiazole amides and biological applications
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, (2018/09/26)
The invention relates to a 5-thiazole amide compound and biology application thereof. The 5-thiazole amide compound has a general formula (I) described in the specification and is used for targeting an AKT/PKB kinase (ATP binding site). Experiments prove that a thiazole amide AKT inhibitor can remarkably inhibit the activity of the AKT kinase in vitro and has strong proliferation inhibition function on various tumor cells with high AKT activity, which indicate that the 5-thiazole amide compound can be used for preparing drugs for resisting tumors.
