Since the PI3K signaling pathway is the most commonly activated in human cancers,inhibition of PI3K is a promising approach to cancer therapy.In this study,a series of 2-methyl-5-nitrobenzeneacylhydrazones were design...Since the PI3K signaling pathway is the most commonly activated in human cancers,inhibition of PI3K is a promising approach to cancer therapy.In this study,a series of 2-methyl-5-nitrobenzeneacylhydrazones were designed and synthesized.All the new derivatives were tested by p110α enzymatic and Rh30 cellular assays.Further enzyme selectivity profiling proved that 6e and 7 were potential selective PI3K inhibitors.展开更多
Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea deri...Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.展开更多
The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Cor...The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Corpus cavernosum.However,the isolation of compound 1 is problematic because of its high similarity in structure to its analogs.In this paper,the first synthesis of 1 was reported featuring two key reactions：a copper-catalyzed coupling reaction and an intramolecular cyclization.展开更多
Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer.In this study,we describe the design,synthesis,and biological evaluation of a series of O-lin...Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer.In this study,we describe the design,synthesis,and biological evaluation of a series of O-linked indoles as potent inhibitors of VEGFR-2.Among these compounds,18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays,with IC50 value of3.8 nmol/L Kinase selectivity profiling revealed that 18 was a multitargeted inhibitor,and it also exhibited good potency against VEGFR-1,PDCFR-α and β.展开更多
基金the National Natural Science Foundation of China(Nos.81273365 and 81321092)Chinese National Science&Technology Major Project "Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09103101-024 and 2014ZX09304002-008-001)+1 种基金Chinese National Programs for High Technology Research and Development(No.2012AA020302)the Shanghai Science and Technology Commission(Nos.11431921100 and 12DZ1930802)for their financial support
文摘Since the PI3K signaling pathway is the most commonly activated in human cancers,inhibition of PI3K is a promising approach to cancer therapy.In this study,a series of 2-methyl-5-nitrobenzeneacylhydrazones were designed and synthesized.All the new derivatives were tested by p110α enzymatic and Rh30 cellular assays.Further enzyme selectivity profiling proved that 6e and 7 were potential selective PI3K inhibitors.
基金the National Natural Science Foundation of China (Nos. 81273365, 81173080, 81321092)National Science & Technology Major Project ‘‘Key New Drug Creation and Manufacturing Program’’ (Nos. 2012ZX09103101-024, 2014ZX09304002-008-001)+1 种基金Chinese National Programs for High Technology Research and Development (No. 2012AA020302)the Shanghai Science and Technology Commission (No. 12DZ1930802) for their financial support
文摘Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.
基金Financial support of the National Natural Science Foundation (Nos.81102461,81021062,and 90813034)National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09301001-001 and 2012ZX09103101-024)the Shanghai Science and Technology Commission(Nos.11431921100 and 12DZ1930802)
文摘The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Corpus cavernosum.However,the isolation of compound 1 is problematic because of its high similarity in structure to its analogs.In this paper,the first synthesis of 1 was reported featuring two key reactions：a copper-catalyzed coupling reaction and an intramolecular cyclization.
基金the National Natural Science Foundation of China (Nos.81273365,81173080 and 81321092)National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09103101-024 and 2014ZX09304002-008-001)+1 种基金Chinese National Programs for High Technology Research and Development(No.2012AA020302)the Shanghai Science and Technology Commission(No. 12DZ1930802) for their financial support
文摘Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer.In this study,we describe the design,synthesis,and biological evaluation of a series of O-linked indoles as potent inhibitors of VEGFR-2.Among these compounds,18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays,with IC50 value of3.8 nmol/L Kinase selectivity profiling revealed that 18 was a multitargeted inhibitor,and it also exhibited good potency against VEGFR-1,PDCFR-α and β.
