Qin, Mingze published the artcileDiscovery of novel diaryl urea derivatives bearing a triazole moiety as potential antitumor agents, Recommanded Product: Methyl 4-chloropicolinate, the main research area is urea triazole antitumor neoplasm; Antitumor activity; Diaryl ureas; Organic synthesis; Structure-activity relationship.
Herein, the authors report a novel series of diaryl urea derivatives bearing a triazole moiety, from which potent antitumor agents have been identified. With a modified triazole, most compounds showed high level activity in both cellular and enzymic assays, accompanied with a suitable ClogD7.4 value. The most active compound, I, effectively suppressed proliferation of HT-29, H460 and MDA-MB-231 cancer cells, with IC50 values of 0.90, 0.85 and 1.54 μM, resp. Compound I also exhibited significant inhibition of tyrosine kinases including c-Kit, RET and FLT3. Furthermore, compound I could obviously induce apoptosis of HT-29 cells in a concentration-dependent manner. The study of structure-activity relationships also revealed that a hydrophilic tail at the 4-position of the triazole was crucial for high activity of the compound
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.