發炎反應(inflammation)為組織受傷或受微生物侵入時的保護反應。
過度或持續的發炎反應與許多疾病的形成有密切關係，其大量表現細胞素 (cytokine)、黏著分子 (adhesion molecules)、生長因子 (growth factor)與分解酵素等等發炎因子，以形成發炎之相關疾病。對抗發炎藥物而言，發炎前驅物質無疑是一個重要的作用目標,一般除了固醇類藥物之外還有NSAIDs (Non-steroidal anti-inflammatory drug)。
由於現有的文獻報告中顯示化合物中具naphthyridinones基團者，有多樣的藥理活性，包括抗發炎、抗微小管聚合等。另外amino-quinazolinone在抗癌的研究方面已發現具有抑制heat shock protein 90、Lck kinase 等作用，顯示此類衍生物具有抗癌活性潛力。藉由找尋抑制Lck kinase，也搜尋到有關aminopyrimidine及其衍生結構具有對MAPK路徑阻斷的作用,並且也有抗發炎潛力。本研究嘗試利用這三種化合物的優點合成phenyldihydro
quinazolinone 為主結構之化合物。
另外合成出phenyldihydroquinazolinone 衍生物，篩選結果顯示，衍生物也對於抗肺癌 (A549)、抗攝護腺癌 (PC3)、胃癌(AGS)、鼻咽癌(TW01)等細胞株具抑制增生活性。
Inflammation is the protective response of the injury or microbialinvasion. Overexpression of the inflammatory response and continuous inflammation is closely related to many diseases.Cytokines, adhesion molecules,growth factors and inflammatory factors,and so a large number of enzymes expressed in many inflammatory reactions and the formation of inflammation-related diseases.Inflammatory hormone agonist is a role of inflammatory drug targets for inflammation and symptoms in addition to steroid drugs alsoNSAIDs.
Shown in the literature of compounds with naphthyridinones moieties have a variety of pharmacological activities,including anti-inflammatory,and antimicrotubule polymerization. On the other hand amino-quinazolinone in cancer research have been found to inhibit Heat shock protein 90(HSP 90), Lck kinase and other effects, such derivatives have shown potential anticancer activity.
To find the path through inhibition of Lck kinase, we also find the relevant aminopyrimidine and its derivativeshave the effect of blocking the MAPK pathway and also has antiinflammatory potential.
We try to use the characteristics of these three compounds,synthesis of phenyldihydroquinazolinone the main frame of the compounds.For cell linessuch as A549,PC3,AGS,TW01, compounds can inhibit the activity of cell line proliferation.
