排序方式: 共有27条查询结果,搜索用时 15 毫秒
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Sonia Gattinoni 《Tetrahedron letters》2007,48(6):1049-1051
The first synthesis of topopyrone C, a natural compound and inhibitor of Topoisomerase I, has been carried out by Marschalk alkylation of 1-hydroxy-3,6,8-trimethoxyanthraquinone, followed by a Baker-Venkataraman chain elongation and an acid-catalyzed cyclization for the construction of the pyrone ring. 相似文献
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Zhen-Gang Li Guo-Qiang Dong Sheng-Zheng Wang Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang Chun-Quan Sheng 《中国化学快报》2015,26(3):267-271
Evodiamine and its derivatives have an asymmetric center at the C13 b position.Herein,isomers of evodiamine derivatives 2 and 3 were obtained by straightforward asymmetric total synthesis.Their inhibitory activities toward topoisomerases I and II and their cytotoxicities in cancer cell lines were evaluated.All the four isomers exhibited good to excellent antitumor potency and the(S)-isomers were generally more active than the(R)-isomers.The binding modes of(S)-2 with topoisomerases I and II were also clarified by molecular docking. 相似文献
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Néstor M. Carballeira David Sanabria Norma L. Ayala Clarisa Cruz 《Tetrahedron letters》2004,45(19):3761-3763
A stereoselective synthesis for the (5Z,9Z)-14-methyl-5,9-pentadecadienoic acid and the monounsaturated analog (Z)-14-methyl-9-pentadecenoic acid was accomplished in six to seven steps where double alkyne coupling was the key step. This synthesis will facilitate the study of the topoisomerase I inhibitory profile of this important class of fatty acids. 相似文献
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Kun Fang Guo-Qiang Dong Hai Gong Na Liu Zhen-Gang Li Shi-Ping Zhu Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang Chun-Quan Sheng 《中国化学快报》2014,25(7):978-982
A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Their capacity to interfere with the catalytic activity of topoisomerase Ⅰ and Ⅱ was evaluated by the relaxation assay. In vitro antitumor activity results revealed that compound 12 showed good antitumor activity with a broad spectrum. Its binding modes with topoisomerase Ⅰ and Ⅱ were clarified by molecular docking. 相似文献
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Friedländer reaction between methyl acetoacetate and 2,4-diaminobenzaldehyde provided quinoline 11. Subsequent tosylation, reduction, silylation, and then oxidation led to aldehyde 15. The latter was subjected to a Pictet-Spengler reaction with tryptophan methyl ester that yielded product 16, and then desilylation gave the lavendamycin analogue 17. This compound was oxidized by Dess-Martin periodinane, and the cyclized derivative 18 was obtained via a hemiaminal intermediate. The same sequence from 2,4-diamino-5-methoxybenzaldehyde or from (2,4-diaminophenyl)propan-3-one led to compounds 30 and 31, or 40 and 41, respectively. 相似文献
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Jun-Peng Zhang Jie Huang Chao Liu Xu-Fang Lu Bao-Xiang Wu Li Zhao Na Lu Qing-Long Guo Zhi-Yu Li Cheng Jiang 《中国化学快报》2014,25(7):1025-1028
A series of new 3-benzoheterocyclic substituted pyridopyrimidines were designed and synthesized. Structures of the compounds were determined by IR, 1H NMR, and elemental analyses. The anti- proliferation activity of 13 novel compounds was evaluated in A549, HL-60, BGC-823 and SMMC-7721 cell lines. Compounds 3, 5, 7, 8, 9,10 showed potent inhibitory activity against the four tested cancer cell lines. These six compounds were examined for Top I inhibition at 100 μmol/L by measuring the relaxation of supercoiled DNA in plasmid pBR322. Most of the tested compounds inhibited the enzyme at this concentration. The most potent compound 9 was as potent as camptothecin. 相似文献
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《Arabian Journal of Chemistry》2019,12(8):2356-2364
A series of 8-(substituted)aryloxycaffeine were prepared from 8-bromocaffeine and (substituted)phenols by modified Ullmann reaction. In vitro antibacterial activity, inhibitory activity on topoisomerase II and pharmacological activities were evaluated for the synthesized 8-(substituted)aryloxycaffeine. Among the synthesized compounds, 8-(5-chloropyridin-3-yloxy)caffeine (3k) showed strong inhibitory activity (MIC = 15.6 μg/mL) against the tested gram negative (−) bacteria Salmonella enteritidis. 8-(quinolin-8-yloxy)caffeine (3g) showed the strongest inhibitory activity against topoisomerase II. And the compounds 8-(6-methylpyridin-2-yloxy)caffeine (3j) and 8-(3-chloro-6-(trifluoromethyl)pyridin-2-yloxy)caffeine (3m) showed analgesic effect without the central nervous system stimulation. 相似文献
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Potential inhibitors of DNA topoisomerase II: ruthenium(II) poly-pyridyl and pyridyl-azine complexes
Manish Chandra D.S. Pandey R.P. Tripathi V.J.M. Reddy Pedro Valerga 《Journal of organometallic chemistry》2004,689(13):2256-2267
In search of new DNA probes a series of new mono and binuclear cationic complexes [RuH(CO)(PPh3)2(L)]+ and [RuH(CO)(PPh3)2(-μ-L)RuH(CO)(PPh3)2]2+ [L=pyridine-2-carbaldehyde azine (paa), p-phenylene-bis(picoline)aldimine (pbp) and p-biphenylene-bis(picoline)aldimine (bbp)] have been synthesized. The reaction products were characterized by microanalyses, spectral (IR, UV-Vis, NMR and ESMS and FAB-MS) and electrochemical studies. Structure of the representative mononuclear complex [RuH(CO)(PPh3)2(paa)]BF4 was crystallographically determined. The crystal packing in the complex [RuH(CO)(PPh3)2(paa)]BF4 is stabilized by intermolecular π-π stacking resulting into a spiral network. Topoisomerase II inhibitory activity of the complexes and a few other related complexes [RuH(CO)(PPh3)2(L)]+ {L=2,4,6-tris(2-pyridyl)-1,3,5-triazine (tptz) and 2,3-bis(2-pyridyl)-pyrazine (bppz)} have been examined against filarial parasite Setaria cervi. Absorption titration experiments provided good support for DNA interaction and binding constants have also been calculated which were found in the range 1.2 × 103-4.01 × 104 M−1. 相似文献