Category: indole-building-block. Zhang, Y; Wang, YY; Zhao, YX; Gu, W; Zhu, YQ; Wang, SF in [Zhang, Yan; Wang, Yunyun; Zhao, Yuxun; Gu, Wen; Wang, Shifa] Nanjing Forestry Univ, Coll Chem Engn, Nanjing 210037, Jiangsu, Peoples R China; [Zhu, Yongqiang] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, Nanjing 210046, Jiangsu, Peoples R China; [Gu, Wen; Wang, Shifa] Nanjing Forestry Univ, Coinnovat Ctr Efficient Proc & Utilizat Forest Re, Nanjing 210037, Jiangsu, Peoples R China published Novel camphor-based pyrimidine derivatives induced cancer cell death through a ROS-mediated mitochondrial apoptosis pathway in 2019.0, Cited 41.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.
A series of novel camphor-based pyrimidine derivatives (3a-3x) have been synthesized; their structures were determined by using conventional methods and compound 3f was further confirmed through single crystal XRD analysis. The cytotoxic activity of the target compounds against a panel of human normal (GES-1) and cancer cell lines (MDA-MB-231, RPMI-8226, A549) was evaluated by MTS assay. Here we found that compound 3f exhibited the strongest anti-tumor activity, comparable to that of etoposide, and had much lower cytotoxicity to normal GES-1 cells (IC50 > 50 mu M) than the reference drug (IC50 = 8.89 mu M). Subsequent mechanism studies in MDA-MB-231 cells revealed that compound 3f caused G0/G1 phase arrest and apoptosis in a dose dependent manner. Moreover, the loss of mitochondrial membrane potential and enhancement of cellular ROS levels were also observed upon 3f treatment, which indicated that 3f exerted cytotoxic activity by a ROS-mediated mitochondrial apoptosis pathway. This result was confirmed by a significant increase in the expression of pro-apoptotic proteins Bax, cytochrome C and caspase-3, and downregulation of anti-apoptosis protein Bcl-2. Overall, 3f can be adopted for further investigation in the development of antitumor agents based on natural products.
Category: indole-building-block. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Zhang, Y; Wang, YY; Zhao, YX; Gu, W; Zhu, YQ; Wang, SF or concate me.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles