Formaldehyde, as one of the simplest reactive carbonyl species（RCS）, is regarded as a potential carcinogen and a sick house syndrome gas. Recent studies have shown that abnormally high levels of formaldehyde may res...Formaldehyde, as one of the simplest reactive carbonyl species（RCS）, is regarded as a potential carcinogen and a sick house syndrome gas. Recent studies have shown that abnormally high levels of formaldehyde may result in cognitive decline and spatial memory deficits, asthmatic symptoms,Alzheimer＇s disease, and cancer. Due to the harmfulness of high levels of formaldehyde in nature and humans, it is of great significance to further elucidate the roles and functions of formaldehyde by a noninvasive detection approach. Fluorescence imaging has become a powerful and popular tool in monitoring bio-species owing to their high sensitivity and selectivity, excellent spatiotemporal resolution and non-invasion nature. Therefore, fluorescent probes are widely applied to track and detect formaldehyde in vitro and in vivo which have attracted more and more interest recently. This review focuses on various strategies to design the fluorescent probes for detecting formaldehyde based on different recognition groups.展开更多
By combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285 with 1,2,3-triazole as linker,eight novel 6-substituted-4-aminoquinazolin derivatives...By combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285 with 1,2,3-triazole as linker,eight novel 6-substituted-4-aminoquinazolin derivatives were synthesized and characterized by -1H NMR,-（13）C NMR,and high resolution mass spectrometry.Their inhibitory activities against five enzymes（VEGFR2,HER2,EGFR,HDAC1,and HDAC6） and five cancer cell lines（A549,BT-474,A431,SK-BR-3,and NCI-H1975） were evaluated.The bioassay results show that the introduction of triazole linked vorinostat-like segment dramatically changed the selectivity profiles of newly synthetic compounds relative to vandetanib,BMS-690514,neratinib,and TAK-285.Among them,compound 6b exerted outstanding enzymatic and cellular activities through its simultaneous and synergistic inhibitions on multiple pathways,which might have the great potential to confer the better benefits than single-targeted inhibitors in cancer therapy.展开更多
基金support from National Natural Science Foundation of China (Nos. 21676113, 21402057, 21472059, 81671803) Youth Chen-Guang Project of Wuhan(2016070204010098)+2 种基金 the 111 Project B17019the Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, Shenzhensupported by self-determined research funds of CCNU from the colleges’ basic research and operation of MOE (No. CCNU16A02004)
文摘Formaldehyde, as one of the simplest reactive carbonyl species（RCS）, is regarded as a potential carcinogen and a sick house syndrome gas. Recent studies have shown that abnormally high levels of formaldehyde may result in cognitive decline and spatial memory deficits, asthmatic symptoms,Alzheimer＇s disease, and cancer. Due to the harmfulness of high levels of formaldehyde in nature and humans, it is of great significance to further elucidate the roles and functions of formaldehyde by a noninvasive detection approach. Fluorescence imaging has become a powerful and popular tool in monitoring bio-species owing to their high sensitivity and selectivity, excellent spatiotemporal resolution and non-invasion nature. Therefore, fluorescent probes are widely applied to track and detect formaldehyde in vitro and in vivo which have attracted more and more interest recently. This review focuses on various strategies to design the fluorescent probes for detecting formaldehyde based on different recognition groups.
基金supported by funding from the National Natural Science Foundation of China(No.21272134)Shenzhen Municipal Government(No.CXB201104210014A and20150113A0410006)
文摘By combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285 with 1,2,3-triazole as linker,eight novel 6-substituted-4-aminoquinazolin derivatives were synthesized and characterized by -1H NMR,-（13）C NMR,and high resolution mass spectrometry.Their inhibitory activities against five enzymes（VEGFR2,HER2,EGFR,HDAC1,and HDAC6） and five cancer cell lines（A549,BT-474,A431,SK-BR-3,and NCI-H1975） were evaluated.The bioassay results show that the introduction of triazole linked vorinostat-like segment dramatically changed the selectivity profiles of newly synthetic compounds relative to vandetanib,BMS-690514,neratinib,and TAK-285.Among them,compound 6b exerted outstanding enzymatic and cellular activities through its simultaneous and synergistic inhibitions on multiple pathways,which might have the great potential to confer the better benefits than single-targeted inhibitors in cancer therapy.
