- Preparation method of apatinib
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The invention provides a preparation method of apatinib. The preparation method comprises that 2-halogenated-3-cyanopyridine as a raw material and 4-aminomethylpyridine undergo a substitution reactionto produce N-(pyridin-4-yl-methyl)-2-amino-3-cyanopyridine, the N-(pyridin-4-yl-methyl)-2-amino-3-cyanopyridine undergoes an esterification reaction to produce N-(pyridin-4-yl-methyl)-2-amino-3-picolinate, and the N-(pyridin-4-yl-methyl)-2-amino-3-picolinate and 1-(4-aminophenyl)cyclopentylformonitrile undergo an amidation reaction to produce apatinib (I). The preparation method has the advantages of low cost and easy availability of raw materials, simple processes, low cost, less waste water generation, safety and environmental protection, easy realization of reaction conditions, high reactivity and selectivity, few side reactions, few apatinib impurities, high purity and high yield.
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- Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines
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Oxadiazole derivatives were synthesized and evaluated for their ability to inhibit tubulin polymerization and to cause mitotic arrest in tumor cells. The most potent compounds inhibited tubulin polymerization at concentrations below 1 μM. Lead analogs caused mitotic arrest of A431 human epidermoid cells and cells derived from multi-drug resistant tumors (10, EC50 = 7.8 nM). Competition for the colchicine binding site and pharmacokinetic properties of selected potent compounds were also investigated and are reported herein, along with structure-activity relationships for this novel series of antimitotic agents.
- Ouyang, Xiaohu,Piatnitski, Evgueni L.,Pattaropong, Vatee,Chen, Xiaoling,He, Hai-Ying,Kiselyov, Alexander S.,Velankar, Avdhoot,Kawakami, Joel,Labelle, Marc,Smith II, Leon,Lohman, Julia,Lee, Sui Ping,Malikzay, Asra,Fleming, James,Gerlak, Jason,Wang, Ying,Rosler, Robin L.,Zhou, Kai,Mitelman, Stan,Camara, Margarita,Surguladze, David,Doody, Jacqueline F.,Tuma, M. Carolina
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p. 1191 - 1196
(2007/10/03)
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- Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors
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A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC 50 values in the single digit nanomolar range. Binding experiments demonstrated that representative
- Ouyang, Xiaohu,Chen, Xiaoling,Piatnitski, Evgueni L.,Kiselyov, Alexander S.,He, Hai-Ying,Mao, Yunyu,Pattaropong, Vatee,Yu, Yang,Kim, Ki H.,Kincaid, John,Smith II, Leon,Wong, Wai C.,Lee, Sui Ping,Milligan, Daniel L.,Malikzay, Asra,Fleming, James,Gerlak, Jason,Deevi, Dhanvanthri,Doody, Jacqueline F.,Chiang, Hui-Hsien,Patel, Sheetal N.,Wang, Ying,Rolser, Robin L.,Kussie, Paul,Labelle, Marc,Tuma, M. Carolina
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p. 5154 - 5159
(2007/10/03)
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