- Norcantharidin carboxylic acid monofluorobenzyl ester and synthesis method and anti-tumor application thereof
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The invention provides synthesis and anti-tumor application of norcantharidin carboxylic acid monofluorobenzyl ester with a structural formula shown as I in the specification. The specific structure of the norcantharidin carboxylic acid monofluorobenzyl ester as shown in the formula I is shown in the specification, and activity tests show that the norcantharidin carboxylic acid monofluorobenzyl ester as shown in the formula I, which is designed and synthesized by the invention, is a suitable anti-tumor candidate drug, especially as an anti-liver cancer candidate drug. Compared with a positivecontrol drug norcantharidin, the norcantharidin sodium salt has the advantage that the water solubility, the stability and the anti-tumor activity are improved. In addition, the synthesis method of norcantharidin carboxylic acid monofluorobenzyl ester has the advantages that the raw materials are easy to obtain, and the operation and the implementation are very easy.
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Paragraph 0028; 0036-0037
(2020/07/02)
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- MOCO/γ-Al2O3-catalyzed hydrodesulfurization to synthesis of cantharidin-based molecules
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In the tubular reactor, Hydrodesulfurization on the 7-ox-9-thiortricyclo[ 32,3.2.2.1]heptanes-5-ene-2,3-dicarboxylica- cid(A) and Nordehydrocantharidin( B) have been accomplished for the first time in the presence of MoCo/γ-Al2O3with the goal of obtaining pharmacologically promising Cantharidin-based molecules. The yields of Cantharidin(C) and Norcantharidin(D) were 71% and 80%. And the structure of compounds C and D was confirmed by 1H-NMR and 13C-NMR, NOESY and ESI-MS. We envisage that this process could be further developed at an industrial scale for the synthesis of Cantharidin-based molecules.
- Du, Hong-Fei,FANG, Ai-Quan,LIU, Xiao-Ling,TAN, Chun-Bin
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p. 305 - 307
(2020/10/06)
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- Camptothecin-glycine-norcantharidin conjugate and application thereof
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The invention provides a camptothecin-glycine-norcantharidin conjugate I and a preparation method thereof. R in the formula I is selected from C1-C6 alkyl groups, substituted alkyl groups, cycloalkylgroups, benzyl groups or substituted benzyl groups. Activity tests prove that the designed and synthesized camptothecin-glycine-norcantharidin conjugate I has an excellent antitumor effect, and especially has high activity on liver cancer, stomach cancer, colon cancer and pancreatic cancer. Additionally, the preparation method of the camptothecin-glycine-norcantharidin conjugate I has the advantages of easily available raw materials, low cost, high yield of the target product, and easiness in preparation.
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Paragraph 0020; 0026; 0027
(2019/12/29)
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- Norcantharidin monoester salt derivative and its anti-tumor application (by machine translation)
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This invention has offered a kind of Norcantharidin monoester salt derivative, its structural formula such as formula 4 shown, Wherein R is selected from C1-C3 alkyl or benzyl; M is selected from positive univalent or divalent cation. Active test proves that, this invention is designed and synthesizing Norcantharidin monoester salt derivative 4 for liver cancer, stomach cancer, colon cancer, and four kinds of tumor colon cancer has good inhibition activity, is expected to be applied to the preparation of the above-mentioned four kinds of anti-tumor drug. (by machine translation)
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Paragraph 0035; 0039; 0040
(2017/04/29)
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- IMPROVED PROCESS FOR THE PREPARATION OF A BENZENE COMPOUND
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A benzene compound is prepared in a process, which comprises (i) reacting a furan compound of formula (I): wherein R1 and R2 are the same or different and independently selected from the group consisting of hydrogen, alkyl, aralkyl, -CHO, -CH2OR3, -CH(OR4 )(OR5), -COOR6, wherein R3, R4 and R5 are the same or different and are independently selected from the group consisting of hydrogen, alkyl, aryl, alkaryl, aralkyl, alkylcarbonyl and arylcarbonyl, or wherein R4 and R5 together form an alkylene group, and wherein R6 is selected from the group consisting of hydrogen, alkyl and aryl, with an olefin of the formula (II): R7-CH=CH-R8; wherein R7 and R8 are the same or different and are independently selected from the group consisting of hydrogen, sulfonate, -CN, -CHO, and -COOR9, wherein R9 is selected from the group consisting of hydrogen, and an alkyl group, or R7 and R8 together form a –C(O)-O-(O)C- group or a –C(O)-NR10-C(O)- group, wherein R10 represents hydrogen, an aliphatic or an aromatic group, to produce an unsaturated bicyclic ether having an unsaturated carbon-carbon bond; (ii) hydrogenating the unsaturated carbon-carbon bond in the unsaturated bicyclic ether to produce a saturated bicyclic ether; and (iii) dehydrating and aromatizing the saturated bicyclic ether to produce the benzene compound.
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Page/Page column 12; 13
(2016/07/05)
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- DEMETHYL-CANTHARIDIN PLATINUM COMPLEX ISOMERS AND THEIR USE
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The present invention provides a stereo-isomer of the demethylcantharidin platinum complex of formula I and use thereof. The stereo-isomer inhibits the growth of cisplatin, carboplatin or oxaliplatin-sensitive and -resistant tumorous cells. The invention also describes a pharmaceutical composition comprising the stereo-isomer of the demethylcantharidin platinum complex and use thereof.
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Page/Page column 5; 6
(2008/06/13)
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- METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF
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Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
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- 7-Oxabicycloheptane- and 7-oxabicycloheptene compounds
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New 7-oxabicycloheptane- and 7-oxabicycloheptene compounds which have the general formula STR1 and intermediates therefor which have the general formulas STR2 are useful as cardiovascular agents.
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