Xu, Qile published the artcileSynthesis and Bioevaluation of 3,6-Diaryl-[1,2,4]triazolo[4,3-b] Pyridazines as Antitubulin Agents, Name: 3-Chloro-6-(3-nitrophenyl)pyridazine, the main research area is triazolo pyridazine preparation antitubulin antiproliferative activity SAR; [1,2,4]Triazolo[4,3-b]pyridazine; colchicine binding site; combretastatin A-4; molecular modeling; tubulin.
A series of 3,6-diaryl-[1,2,4]triazolo[4,3-b]pyridazines were designed as a class of vinylogous CA-4 analogs. The easily isomerized (Z,E)-butadiene linker of vinylogous CA-4 was replaced by a rigid [1,2,4]triazolo[4,3-b]pyridazine scaffold. Twenty-one target compounds were synthesized and exhibited moderate to potent antiproliferative activity. The compound with a 3-amino-4-methoxyphenyl moiety as the B-ring, comparable to CA-4 (IC50 = 0.009-0.012 μM), displayed the highly active antiproliferative activity against SGC-7901, A549, and HT-1080 cell lines with IC50 values of 0.014, 0.008, and 0.012 μM, resp. Tubulin polymerization experiments indicated that it effectively inhibited tubulin polymerization, and immunostaining assay revealed that it significantly disrupted tubulin microtubule dynamics. Moreover, cell cycle studies revealed that this compound dramatically arrested cell cycle progression at G2/M phase in A549 cells. Mol. modeling studies showed that it could bind to the colchicine binding site on microtubules.
ACS Medicinal Chemistry Letters published new progress about Antiproliferative agents. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Name: 3-Chloro-6-(3-nitrophenyl)pyridazine.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem