近年来,由于越来越多的证据表明查尔酮及其衍生物具有抗肿瘤和抗癌功效,因此已成为全球科学家关注的焦点。在这里,我们本研究中设计和合成的查耳酮衍生自萘醛和苯乙酮的衍生物。据报道,这两种前体都表现出一定程度的抗癌特性。此外,这些前体上的取代基如羟基、甲氧基、异戊二烯基和氯也被证明能够增强抗癌效率。因此,当前研究的兴趣是研究由这些具有不同烷氧基取代基和有或没有氟部分的前体组成的杂化分子(查尔酮)的抗癌潜力。设计、合成了两个系列的查耳酮衍生物,并使用元素分析、IR、1 H 和13 C NMR 光谱进行表征,随后评估了它们的抗癌活性。有趣的是,结果表明,与非氟化查耳酮衍生物相比,氟化查耳酮11-15对乳腺癌细胞系 (4T1) 表现出更强的细胞毒活性。值得注意的是,这些氟化查耳酮衍生物对乳腺癌 4T1 细胞系的选择性指数高于顺铂,顺铂是当前医疗实践中最常用的化疗药物之一。这些发现可以让我们深入了解氟化查耳酮作为抗癌剂的潜力,该抗癌剂在
SUBSTITUTED METHYLENE AMIDE DERIVATIVES AS MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPS)
申请人:Applied Research Systems ARS Holding N.V.
公开号:EP1470102A1
公开(公告)日:2004-10-27
[EN] SUBSTITUTED METHYLENE AMIDE DERIVATIVES AS MODULATORS OF PROTEIN TYROSINE PHOSPHATASES PTPS<br/>[FR] DERIVES AMIDES SUBSTITUES METHYLENE EN TANT QUE MODULATEURS DE PROTEINE TYROSINE PHOSPHATASES (PTP)
申请人:APPLIED RESEARCH SYSTEMS
公开号:WO2003064376A1
公开(公告)日:2003-08-07
The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).