微管类药物在转移、耐药的癌症治疗中发挥重要的作用。然而,临床上出现微管类药物耐药现象,需要研究者研发具有新作用模式、新机制的分子来克服耐药问题。多靶点药物分子策略是近年来针对复杂性疾病及耐药问题发展起来的一种药物分子设...微管类药物在转移、耐药的癌症治疗中发挥重要的作用。然而,临床上出现微管类药物耐药现象,需要研究者研发具有新作用模式、新机制的分子来克服耐药问题。多靶点药物分子策略是近年来针对复杂性疾病及耐药问题发展起来的一种药物分子设计策略。本文在替巴尼布林基础上,结合课题组前期研究,开展微管蛋白(tubulin)及原癌基因酪氨酸蛋白激酶Src(proto-oncogene tyrosine protein kinase Src,c-Src)双靶点抑制剂研究。从增加饱和碳原子比率(fraction of sp^(3)-hybridized carbon atoms,Fsp^(3))角度出发,合成16个目标化合物,并通过核磁共振氢谱、碳谱和质谱对其结构进行表征;采用噻唑蓝(MTT)法评价了化合物对宫颈癌细胞(HeLa)和肝癌细胞(HepG2)两种细胞株的生长抑制活性,并通过免疫荧光和流式细胞术评价化合物22对微管和细胞周期的影响。结果显示2-咪唑啉酮不适合替代替巴尼布林中的吡啶结构,化合物22对HeLa和HepG2的半数生长抑制浓度分别为45和51 nmol·L^(-1),并且能够破坏微管结构,将细胞周期阻滞于G2/M期。化合物22可作为先导物开展进一步深入研究。展开更多
The novel structures of organometallic compounds 3-biaryl-1-ferrocenyl-2-propene- 1-ones 5 were synthesized for nonlinear optical chromophores by Suzuki cross-coupling reaction. Their structures were determined with ...The novel structures of organometallic compounds 3-biaryl-1-ferrocenyl-2-propene- 1-ones 5 were synthesized for nonlinear optical chromophores by Suzuki cross-coupling reaction. Their structures were determined with elemental analyses, 1H NMR spectra and 13C NMR spectra.展开更多
A series of symmetrical biaryls was synthesized from arylmercuric chlorides and biarylmercurials in the presence of [ClRh(CO) 2] 2 in hexamethylphosphoramide(HMPA). The mechanism of the [ClRh(CO) 2] 2 catalyzed d...A series of symmetrical biaryls was synthesized from arylmercuric chlorides and biarylmercurials in the presence of [ClRh(CO) 2] 2 in hexamethylphosphoramide(HMPA). The mechanism of the [ClRh(CO) 2] 2 catalyzed dimerization of biarylmercurials was studied, and shown to be mainly intermolecular reaction.展开更多
In the case of Pd(PPh3)4 as catalyst and toluene as reaction solvent, the desired biaryls and polyaryls were synthesized in excellent yield and on a large scale.
Various functionalized asymmetrical biaryls can be synthesized in high to excellent yields via coupling reaction of aryl iodides or bromides with NaBPh4 catalyzed by MCM-41-supported sulfur palladium（0） complex. Thi...Various functionalized asymmetrical biaryls can be synthesized in high to excellent yields via coupling reaction of aryl iodides or bromides with NaBPh4 catalyzed by MCM-41-supported sulfur palladium（0） complex. This palladium complex can be easily recovered and reused many times without loss of activity.展开更多
The novel organometallic compounds, 3-[4'(or 2')-(4''-fluorophenyl)] phenyl-1-ferroc- enyl-2-propen-1-ones 5 were synthesized for nonlinear optical chromophores by Pd (0) catalyzed Suzuki cross-coupl...The novel organometallic compounds, 3-[4'(or 2')-(4''-fluorophenyl)] phenyl-1-ferroc- enyl-2-propen-1-ones 5 were synthesized for nonlinear optical chromophores by Pd (0) catalyzed Suzuki cross-coupling reaction. Their structures were established with elemental analysis, MS, IR and H NMR spectroscopies. 1展开更多
Peptide nanofibers decorated with palladium nanoparticles catalyzed direct coupling of aryl halides with hydroxybenzotriazole to afford the corresponding biaryls in good to excellent yields.The coupling reactions proc...Peptide nanofibers decorated with palladium nanoparticles catalyzed direct coupling of aryl halides with hydroxybenzotriazole to afford the corresponding biaryls in good to excellent yields.The coupling reactions proceeded under simple,green,and mild conditions.The peptide nanofibers were used as recyclable supports in the coupling reactions.This approach is the first to use hydroxybenzotriazole as a phenylating agent.展开更多
文摘微管类药物在转移、耐药的癌症治疗中发挥重要的作用。然而,临床上出现微管类药物耐药现象,需要研究者研发具有新作用模式、新机制的分子来克服耐药问题。多靶点药物分子策略是近年来针对复杂性疾病及耐药问题发展起来的一种药物分子设计策略。本文在替巴尼布林基础上,结合课题组前期研究,开展微管蛋白(tubulin)及原癌基因酪氨酸蛋白激酶Src(proto-oncogene tyrosine protein kinase Src,c-Src)双靶点抑制剂研究。从增加饱和碳原子比率(fraction of sp^(3)-hybridized carbon atoms,Fsp^(3))角度出发,合成16个目标化合物,并通过核磁共振氢谱、碳谱和质谱对其结构进行表征;采用噻唑蓝(MTT)法评价了化合物对宫颈癌细胞(HeLa)和肝癌细胞(HepG2)两种细胞株的生长抑制活性,并通过免疫荧光和流式细胞术评价化合物22对微管和细胞周期的影响。结果显示2-咪唑啉酮不适合替代替巴尼布林中的吡啶结构,化合物22对HeLa和HepG2的半数生长抑制浓度分别为45和51 nmol·L^(-1),并且能够破坏微管结构,将细胞周期阻滞于G2/M期。化合物22可作为先导物开展进一步深入研究。
文摘The novel structures of organometallic compounds 3-biaryl-1-ferrocenyl-2-propene- 1-ones 5 were synthesized for nonlinear optical chromophores by Suzuki cross-coupling reaction. Their structures were determined with elemental analyses, 1H NMR spectra and 13C NMR spectra.
基金Supported by the Scientific Research Foundation for Returned Overseas Chinese Scholarsof Educational Ministry ofChina
文摘A series of symmetrical biaryls was synthesized from arylmercuric chlorides and biarylmercurials in the presence of [ClRh(CO) 2] 2 in hexamethylphosphoramide(HMPA). The mechanism of the [ClRh(CO) 2] 2 catalyzed dimerization of biarylmercurials was studied, and shown to be mainly intermolecular reaction.
基金Support from the University of Science and Technology of China the National Natural Science Foundation of China are gratefully acknowledged (NO. 50073021).
文摘In the case of Pd(PPh3)4 as catalyst and toluene as reaction solvent, the desired biaryls and polyaryls were synthesized in excellent yield and on a large scale.
基金National Natural Science Foundation of China （Project 20462002） Natural Science Foundation of Jiangxi Province （Project 0420015） for financial support.
文摘Various functionalized asymmetrical biaryls can be synthesized in high to excellent yields via coupling reaction of aryl iodides or bromides with NaBPh4 catalyzed by MCM-41-supported sulfur palladium（0） complex. This palladium complex can be easily recovered and reused many times without loss of activity.
文摘The novel organometallic compounds, 3-[4'(or 2')-(4''-fluorophenyl)] phenyl-1-ferroc- enyl-2-propen-1-ones 5 were synthesized for nonlinear optical chromophores by Pd (0) catalyzed Suzuki cross-coupling reaction. Their structures were established with elemental analysis, MS, IR and H NMR spectroscopies. 1
基金the Research Facility of Ilam University,Ilam,Iran,for financial support of this research project
文摘Peptide nanofibers decorated with palladium nanoparticles catalyzed direct coupling of aryl halides with hydroxybenzotriazole to afford the corresponding biaryls in good to excellent yields.The coupling reactions proceeded under simple,green,and mild conditions.The peptide nanofibers were used as recyclable supports in the coupling reactions.This approach is the first to use hydroxybenzotriazole as a phenylating agent.
