A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The struct...A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The structures of these derivatives were characterized by H-RMS and NMR analysis. X-ray crystallography showed that 3 a is in a monoclinic system, space group of P21/c with a = 13.0464(16), b = 12.6244(16), c = 20.210(3)A,β= 105.215(2)o, V =3211.9(7)A^3, Z = 4, F(000)= 1352,μ= 0.42 mm^–1, S = 1.07, the final R = 0.059 and wR = 0.195.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activity against these cell lines.展开更多
In order to discover the novel antitumor agents,a series of N,N,1-triphenyl-1Hbenzo[d]imidazol-5-amine derivatives were designed and synthesized,and the structures were characterized by IR,H-RMS,1H and 13C NMR.X-ray c...In order to discover the novel antitumor agents,a series of N,N,1-triphenyl-1Hbenzo[d]imidazol-5-amine derivatives were designed and synthesized,and the structures were characterized by IR,H-RMS,1H and 13C NMR.X-ray crystallography showed that 4c is in monoclinic system,space group P1 with a=9.209(2),b=9.533(3),c=14.097(3)?,β=102.069(3)°,V=1202.2(5)?3,Z=2,F(000)=528,μ=1.74 mm–1,S=1.024,the final R=0.0448 and wR=0.1109.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer cell lines K562,HL-60,HeLa and BGC-823.The target compounds demonstrated weak or moderate antitumor activities against these cell lines.展开更多
基金Supported by the foundation of the Department of Education of Guangdong Province(2016KTSCX144,2017KZDXM085)Natural Science Foundation of Hunan Province(No.2018JJ3196)the High-level Scientific Research Foundation for the introduction of talent(AL2018008)
文摘A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The structures of these derivatives were characterized by H-RMS and NMR analysis. X-ray crystallography showed that 3 a is in a monoclinic system, space group of P21/c with a = 13.0464(16), b = 12.6244(16), c = 20.210(3)A,β= 105.215(2)o, V =3211.9(7)A^3, Z = 4, F(000)= 1352,μ= 0.42 mm^–1, S = 1.07, the final R = 0.059 and wR = 0.195.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activity against these cell lines.
基金Supported by the “Climbing Program”(pdjh2019b0497)Special Funds,the Foundation of the Department of Education of Guangdong Province(2018KZDXM070,2017KZDXM085,2017KQNCX204)College Students Innovation and Entrepreneurship Training Program of Wuyi University and Foundation for Young Talents(2018KQNCX272,2018KQNCX273)
文摘In order to discover the novel antitumor agents,a series of N,N,1-triphenyl-1Hbenzo[d]imidazol-5-amine derivatives were designed and synthesized,and the structures were characterized by IR,H-RMS,1H and 13C NMR.X-ray crystallography showed that 4c is in monoclinic system,space group P1 with a=9.209(2),b=9.533(3),c=14.097(3)?,β=102.069(3)°,V=1202.2(5)?3,Z=2,F(000)=528,μ=1.74 mm–1,S=1.024,the final R=0.0448 and wR=0.1109.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer cell lines K562,HL-60,HeLa and BGC-823.The target compounds demonstrated weak or moderate antitumor activities against these cell lines.
