Sana, Sravani published the artcileCinnamide derived pyrimidine-benzimidazole hybrids as tubulin inhibitors: Synthesis, in silico and cell growth inhibition studies, Recommanded Product: 2-Amino-4,6-dichloropyrimidine, the publication is Bioorganic Chemistry (2021), 104765, database is CAplus and MEDLINE.
A new class of piperazine-linked cinnamide derivatives of benzimidazole-pyrimidine hybrids have been synthesized and their in vitro cytotoxicity profiles were explored on selected human cancer cell lines. Specifically, structural comparison of target hybrids with tubulin-DAMA-colchicine and tubulin-nocodazole complexes has exposed a deep position of benzimidazole ring into the αT5 loop. The utmost cytotoxicity has shown with an amine linker of benzimidazole-pyrimidine series, with toward A549 (lung cancer) cell line. The most potent compound in this series was 18i, which inhibited cancer cell growth at micromolar concentrations ranging 2.21-7.29μM. Flow cytometry studies disclosed that compound I inhibited the cells in G2/M phase of cell cycle. The most active compound I also inhibited tubulin polymerization with an IC50 of 5.72 ± 0.51μM. In vitro biol. anal. of compound I presented apoptosis induction on A549 cells with triggering of ROS generation and loss of mitochondrial membrane potential, resulting in DNA injury. In addition, compound I displayed impairment in cellular migration and inhibited the colony formation. Notably, the safety profile of most potent compound 18i was revealed by screening against normal human pulmonary epithelial cells (L132: IC50: 69.25 ± 5.95μM). The detailed binding interactions of compound I with tubulin was investigated by employing mol. docking, superimposition and free energy analyses.
Bioorganic Chemistry published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Recommanded Product: 2-Amino-4,6-dichloropyrimidine.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia