Anti-proliferative and migratory inhibition study of b16f10 in mouse melanoma cells induced by synthetic indole-oxadiazole bearing butanamides

M. Abbasi, Seong-Hui Eo, A. Rehman, S. Z. Siddiqui, Yohan Han, Seon-Mi Yu, Song-Ja Kim, Mubashir Hassan, H. Raza, S. A. Shah, S. Seo, Bandar Puncak Alam Selangor Darul Ehsan Malaysia. Puncak Alam Campus
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Abstract

Matrix metalloproteinases-2 and -9 (MMP-2/-9) are key tissue remodeling enzymes that have multiple overlapping activities critical for wound healing and tumor progression. In search of new anti-tumor agents, indole-oxadiazole containing butanamides (1-5) were evaluated with B16F10 mouse melanoma cells in this study. The results showed that compounds 1, 2 and 3 inhibited the cell proliferation in a considerable manner at concentrations ranging from 0-44 ?M. The possible migration inhibitory effects of these melanoma cells were further evaluated through gelatinolytic activity of MMP-2 and MMP-9 secreted from B16F10 cells and it was inferred that compounds 1, 2 and 3 affected the expression and activity of these enzymes in a dose dependent manner while compound 1 can be regarded as promising anti-tumor agent.
合成含吲哚-恶二唑丁烷酰胺诱导小鼠黑色素瘤细胞b16f10的抗增殖和迁移抑制研究
基质金属蛋白酶-2和-9 (MMP-2/-9)是关键的组织重塑酶,具有多种重叠活性,对伤口愈合和肿瘤进展至关重要。为了寻找新的抗肿瘤药物,本研究用B16F10小鼠黑色素瘤细胞对含丁酰胺(1-5)的吲哚-恶二唑进行了评价。结果表明,化合物1、2和3在0 ~ 44 μ M浓度范围内对细胞增殖有明显的抑制作用。通过B16F10细胞分泌的MMP-2和MMP-9的溶胶活性进一步评价了这些黑色素瘤细胞可能的迁移抑制作用,推断化合物1、2和3影响这些酶的表达和活性呈剂量依赖性,而化合物1可以视为有前景的抗肿瘤药物。
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