99009-20-8 吡唑并吖啶

名称和标识

中文名: 吡唑并吖啶
英文名: Pyrazoloacridine
CAS号: 99009-20-8
分子式: C19H21N5O3
分子量: 367.4
中文别名: 化合物T28475; 化合物PYRAZOLOACRIDINE
英文别名: Pyrazolo(3,4,5-kl)acridine-2(6H)-propanamine, N,N-dimethyl-9-methoxy-5-nitro-; (3-(9-METHOXY-5-NITRO-6H-PYRAZOLO(3,4,5-KL)ACRIDIN-2-YL)-PROPYL)-DIMETHYL-AMINE; 2,6-Dihydro-2-(3-dimethylaminopropyl)-9-methoxy-5-nitropyrazolo[3,4,5-kl]acridine; 9-Methoxy-N,N-dimethyl-5-nitropyrazolo[3,4,5-kl]acridine-2(6H)-propane-1-amine; 1,2,6,10b-Tetrahydro-5-nitro-9-methoxy-2-[3-(dimethylamino)propyl]pyrazolo[3,4,5-kl]acridine; NSC 366140

用途与制备

生物活性 Pyrazoloacridine (NSC 366140) 具有抗癌活性，抑制拓扑异构酶 1 和 2 的活性 (topoisomerases 1 and 2)。Pyrazoloacridine (NSC 366140) 对 K562 髓系白血病细胞中的 IC50 值为 1.25 μM (24 h)。
体外研究 Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC 50 values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells. Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro. Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer. Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells. Pyrazoloacridine (NSC 366140) induces apoptosis in P53-deficient Hep 3B human hepatoma cells. Cell Cytotoxicity Assay Cell Line: K562 Myeloid Leukemia Cells. Concentration: 0-500 μM. Incubation Time: 1 h or 24 h. Result: When K562 cells were incubated with PA for 1 h and then plated in soft agar, an IC 50 of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC 50 was 1.25 μM.

医药

词条详情加载中…