具有高抗乳腺癌细胞细胞毒性活性的新型β-咔啉基查耳酮的合成。
Synthesis of novel β-carboline based chalcones with high cytotoxic activity against breast cancer cells.
作者信息
Chauhan Shikha S, Singh Anup K, Meena Sanjeev, Lohani Minaxi, Singh Akhilesh, Arya Rakesh K, Cheruvu Srikanth H, Sarkar Jayanta, Gayen Jiaur R, Datta Dipak, Chauhan Prem M S
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India; Department of Chemistry, Integral University, Lucknow 226 026, U.P., India.
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
出版信息
Bioorg Med Chem Lett. 2014 Jul 1;24(13):2820-4. doi: 10.1016/j.bmcl.2014.04.109. Epub 2014 May 4.
A series of novel β-carboline based chalcones was synthesized and evaluated for their cytotoxic activity against a panel of human cancer cell lines. Among them we found that two of the compounds 7c and 7d, showed marked anti-proliferative activity in a panel of solid tumor cell lines with highest effect in breast cancer. The compounds 7c and 7d showed an IC50 of 2.25 and 3.29 μM, respectively against human breast cancer MCF-7 cell line. Further, the compound 7c markedly induced DNA fragmentation and apoptosis in breast cancer cells.
合成了一系列基于新型β-咔啉的查耳酮，并评估了它们对一组人类癌细胞系的细胞毒性活性。其中，我们发现化合物7c和7d中的两种在一组实体瘤细胞系中表现出显著的抗增殖活性，对乳腺癌的效果最为显著。化合物7c和7d对人乳腺癌MCF-7细胞系的IC50分别为2.25和3.29 μM。此外，化合物7c在乳腺癌细胞中显著诱导DNA片段化和凋亡。
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