Structure activity relationship, cytotoxicity and evaluation of antioxidant activity of curcumin derivatives

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• 作者：Pramod K. Sahu^a ; ^b ; ^{sahu.chemistry@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; ^{researchdata6@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Praveen K. Sahu^b ; Puran L. Sahu^c ; Dau D. Agarwal^a ; ^b
• 关键词：Antioxidant activity ; Cytotoxicity ; Structure&ndash ; activity relationship ; Curcumin derivatives/analogues
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：26
• 期：4
• 页码：1342-1347
• 全文大小：676 K

文摘

Series of curcumin derivatives/analogues were designed and efficient method for synthesis thereof is described. All the synthesized compounds have been screened for their cytotoxicity and evaluated their antioxidant activity. Cytotoxicity effect has been evaluated against three cell lines Hep-G2, HCT-116 and QG-56 by MTT assay method. Structure activity relationship has revealed that particularly, compound 3c, (IC₅₀ value 6.25 μM) has shown better cytotoxicity effect against three cell lines. According to results of SAR study, it was found that 4H-pyrimido[2,1-b]benzothiazole derivatives (2e and 2f), pyrazoles (3a, 3b, 3c and 3d) benzylidenes (4d) exhibited better antioxidant activity than curcumin. A correlation of structure and activities relationship of these compounds with respect to drug score profiles and other physico-chemical properties of drugs are described and verified experimentally.