590-67-0, Name is 1-Methylcyclohexanol, molecular formula is C7H14O, Computed Properties of C7H14O, belongs to benzoxazole compound, is a common compound. In a patnet, author is Yuan, Xu, once mentioned the new application about 590-67-0.
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase
Herein, we have carried out a structural optimization campaign to discover the novel anti-tumor agents with our previously screened YQY-26 as the hit compound. A library of thirty-seven 6-amide-2-aryl benzoxazole/benzimidazole derivatives has been designed and synthesized based on the highly conserved active site of VEGFR-2. Several title compounds exhibited selective inhibitory activities against VEGFR-2 than EGFR kinases, which also displayed selective anti-proliferation potency against the HUVEC and HepG2 than the A549 and MDA-MB-231 cancer cell lines. The newly synthesized compounds were evaluated for anti-angiogenesis capability by chick chorioallantoic membrane (CAM) assay. Among them, compounds 9d showed the most potent anti-angiogenesis ability (79% inhibition at 10 nM/eggs), the efficient cytotoxic activities (in vitro against the HUVEC and HepG2 cell lines with IC50 values of 1.47 and 2.57 mu M, respectively), and excellent VEGFR-2 kinase inhibition (IC50 = 0.051 mu M). The molecular docking analysis revealed that compound 9d is a Type 11 inhibitor of VEGFR-2 kinase. These results indicated that the 6-amide-2-arylbenzoxazole and 6-amide-2-aryl benzimidazole derivatives are promising inhibitors of VEGFR-2 kinase for the potential treatment of anti-angiogenesis. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem