- Cyclohexadienones-insect growth inhibitors from the foliar surface and tissue extracts of Senecio cannabifolius
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Dewaxed leaf surface extracts of 12 plants from Hokkaido, prepared by dipping fresh leaves in chloroform for 3 min, were used in a choice leaf-disk bioassay against larvae of the tobacco cutworm Spodoptera litura. Activity was found only in the extract of
- Lajide,Escoubas,Mizutani
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- Synthesis and biological evaluations of cytotoxic and antiangiogenic triterpenoids-jacaranone conjugates
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Background: The development of antiangiogenic agents arises as a more effective and selective therapeutic approach for the treatment of cancer. In addition to reduced acute toxicity, the efficacy of chemotherapy could be improved when administered in combination specific antiangiogenic with cytotoxic agents. The conjugation or hybridization of bifunctional molecules is one of the alternative rational design strategies for co-administration of anticancer drugs. Objective and Methods: The goal of this work is to prepare the conjugates of an antiangiogenic triterpene, 3-oxo oleanolic acid, and structurally related triterpenoids with a cytotoxic semibenzoquinone, jacaranone. The cytotoxic, antiproliferative and antiangiogenic activities of segments and conjugates were determined. The possible targets of conjugates 6a-6h were predicted using Similarity Ensemble Approach (SEA). Results: The results showed that these conjugates are more potent in both cytotoxic and antiangiogenic assays than their corresponding parent molecules, and are also selectively more active against melanoma cells B16 and metastatic B16BL6 than the two other cancer cell lines (A549 and MCF-7) tested. The predicted antiangiogenesis related targets could involve glycogen phosphorylase, neuraminidase, interferon gamma, and tubulin beta chain. Conclusion: The bifunctional conjugates could be useful as dual acting antitumor/antigiogenic agents.
- Sun, Hua,Yue, Partick Y.K.,Wang, Shao-Rong,Huo, Lihong,Zhao, Ying,Xie, Songbo,Kringelum, Jens V.,Lund, Ole,Taboureau, Olivier,Zhou, Jun,Wong, Ricky N. S.,Fang, Wei-Shuo
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p. 775 - 785
(2016/11/29)
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- Regioselective reaction of quinones with Reformatsky reagent: (BrZnCH 2CO2Et·THF)2
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Reformatsky reactions of p-quinones with crystalline reagent (BrZnCH 2CO2Et·THF)2 were investigated and took place successfully, providing β-hydroxy esters in high yield. Notably, in the case of 2,6-disubstituted-p-quinone
- Kawakami, Jun-Ichi,Nakamoto, Koji,Nuwa, Shigeru,Handa, Syoji,Miki, Shokyo
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p. 1201 - 1203
(2007/10/03)
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- PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME
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The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5·THF)2.
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- Convenient Synthesis of Quinol Esters by Indium-mediated Reformatsky reaction of Quinones
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Indium-mediated Reformatsky reaction of para-quinones gives good yields of para-quinols under mild conditions.Naturally occuring quinol esters such as jacaranone are conveniently prepared in a one-pot synthesis.
- Araki, Shuki,Katsumura, Nobuhito,Kawasaki, Ken-ichi,Butsugan, Yasuo
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p. 499 - 500
(2007/10/02)
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