脱氢姜酮类似物在合成有吸引力的磺酰胺类化合物中的潜在抗肿瘤作用

Jovana Muskinja, Z. Ratković, S. Popovic, Sanja Matic, D. Todorović, D. Baskić
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引用次数: 0

摘要

磺胺类化合物是设计具有潜在生物活性化合物的重要支架。它们是几组药物的基础,可以被称为磺胺类药物。从这一事实出发,我们想用天然产物香兰素的衍生物合成一些新型磺胺类化合物。在此基础上,我们合成了脱氢姜酮、4-(4-羟基-3-甲氧基苯基)-3-丁烯-2-酮及其烷基衍生物。这些化合物是合成新的磺胺类化合物的良好底物。新化合物的结构通过红外光谱和核磁共振光谱进行了表征。处理48h后,采用比色MTT法检测14种新有机化合物对SW480、Hela和MRC-5的细胞毒性。细胞毒性比(CR)计算为每种化合物对正常细胞的细胞毒性百分比和相同化合物对肿瘤细胞系的细胞毒性百分比。CR指出,一些新的化合物有希望进行进一步的实验。
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Dehydrozingerone analogues in synthesis attractive sulfonamide compounds as potential antitumor agents
Sulfonamides are very important scaffold in design of different compounds with potential biological activity. They are the basis of several groups of drugs and could be called sulfa drugs. Starting from this fact, we wanted to synthesize some new types of sulfonamides, prepared from derivatives of natural product vanillin. In light of this, we synthesized dehydrozingerone, 4-(4-hydroxy-3-methoxyphenyl)-3-buten-2-one, and its alkyl derivatives. These compounds served as good substrates in the synthesis of new sulfonamide compounds. The structures of the new compounds were determined by IR and NMR methods. Cytotoxicity screening of fourteen new organic compounds against SW480, Hela and MRC-5 was measured by colorimetric MTT assay after 48h of treatment. Cytotoxicity ratio (CR) was calculated as % of cytotoxicity of each compound on normal cells and % of cytotoxicity of the same compounds on tumor cell line. CR is pointed to some new compounds as promising candidates for further experiments.
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