piperidines has been researched along with 2-4-diaminopyrimidine* in 2 studies
2 other study(ies) available for piperidines and 2-4-diaminopyrimidine
| Article | Year |
|---|---|
Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors.
The Aurora kinases are a family of serine/threonine kinases that interact with components of the mitotic apparatus and serve as potential therapeutic targets in oncology. Here we synthesized 15 2,4-diaminopyrimidines and evaluated their biological activities, including antiproliferation, inhibition against Aurora kinases and cell cycle effects. These compounds generally exhibited more potent cytotoxicity against tumor cell lines compared with the VX-680 control, especially compound 11c, which showed the highest cytotoxicities, with IC50 values of 0.5-4.0 μM. Compound 11c had more than 35-fold more selectivity for Aurora A over Aurora B, and molecular docking analysis indicated that compound 11c form better interaction with Aurora A both from the perspective of structure and energy. Furthermore, compound 11c induced G2/M cell cycle arrest in HeLa cells. This series of compounds has the potential for further development as selective Aurora A inhibitors for anticancer activity. Topics: Aurora Kinase A; Aurora Kinase B; Cell Cycle; Cell Proliferation; Enzyme-Linked Immunosorbent Assay; Flow Cytometry; HeLa Cells; Humans; Immunoblotting; Molecular Docking Simulation; Piperazines; Piperidines; Protein Kinase Inhibitors; Pyrimidines | 2015 |
One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties.
A series of novel 2,4-diaminopyrimidines containing piperidine and piperazine moieties were synthesized via an efficient one-pot methodology. The bioassay tests demonstrated that compounds 27 and 28 displayed much stronger antitumor activities against four human cancer cell lines (HepG2, A549, MDA-MB-231 and MCF-7) than positive control fluorouracil. Particularly, compound 28 showed a two-fold improvement compared to fluorouracil in inhibiting MDA-MB-231 and A549 cell proliferation with IC50 values of 7.46 and 12.78 μM, respectively. Further flow-activated cell sorting analysis revealed that the most promising compound 28 displayed a significant effect on G2/M cell-cycle arrest in a dose-dependent manner in MDA-MB-231 cells. Topics: Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Hep G2 Cells; Humans; MCF-7 Cells; Molecular Structure; Piperazine; Piperazines; Piperidines; Pyrimidines; Structure-Activity Relationship | 2014 |