- New modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment
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The similarity of spatial structure between radicicol and matrine urged us to perform conformation modification of matrine, followed by L-shaped matrine derivatives, 6, 12, 21a-h and 22a-h were originally designed, synthesized and evaluated for Hsp90N inhibitors as anticancer agents. TSA (Thermal Shift Assay) results indicated that 21e, 22a-c and 22e-g exhibited strong binding force against Hsp90N with∣ΔTm∣ > 3, meanwhile, MTT assay also revealed these compounds displayed potent anticancer activity with IC50 values below 25 μM against HepG2, HeLa and MDA-MB-231 cells lines. Then, compound 22g with a high ΔTm = 10.92 was chosen as a representative to perform further mechanism study. It can induce cell apoptosis, arrest the cell cycle at the S phase and decrease the expression level of Hsp90 in Hela cell. These results originally provided targeted modification strategy for matrine derivatives to serve as Hsp90 inhibitors for cancer therapy.
- Cao, Huiling,Jing, Dewang,Wang, Haodong,Wang, Lisheng,Wu, Yongji,Xing, Lu,Xu, Yiming,Zhao, Dong,ur Rashid, Haroon
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- Controllable and efficient oxidation of thioether by 2-iodoxybenzoic acid (IBX) in water: Semisynthesis of sophocarpine
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A metal-free, environment friendly, easy-to-operate, and efficient method for the semisynthesis of sophocarpine from matrine has been developed in an overall yield of 91%. The route features a controllable and efficient oxidation of thioether to sulfoxide by 2-iodoxybenzoic acid (IBX) in water.
- Li, Chaojie,Liu, Yuxiu,Wang, Qingmin
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- Synthesis and biological evaluation of the matrine derivatives as a novel family of potential anticancer agents
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Background: ‘FufangKushen injection’ was a Chinese Traditional anticancer drug, which has been widely used to treat cancer in combination with other anticancer drugs. Objective: Our goal is to synthesize a series of novel 13-dithiocarbamates matrine deriv
- Wang, Jing,Liu, Hang,Zhuo, Xiao-Bin,Ye, Guang-Ming,Zhao, Qing-Jie
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p. 493 - 500
(2021/03/26)
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- A method for synthesizing sophocarpine
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The invention provides a new method for synthesizing sophocarpine. The method comprises the following steps: removing alpha-position hydrogen in amide in matrine by taking matrine as a raw material and taking lithium diisopropylamide (LDA) as alkali, then directly performing nucleophilic substitution reaction with diphenyl disulfide to obtain 14-thiophenyl matrine, oxidizing by IBX (o-iodyl-benzoic acid) in a water phase to obtain 14-phenylsulfinyl matrine and eliminating benzenesulfenic acid under the assistance of weak alkali to obtain sophocarpine. The method provided by the invention takes the step of oxidizing a nitrogen-containing thioether compound with IBX in a water phase to form sulfoxide as the key step for synthesizing sophocarpine. The method is characterized by high efficiency, environmental friendliness and easiness in operation. The synthesis route is as shown in the description.
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- Controllable and efficient oxidation of thioether by 2-iodoxybenzoic acid (IBX) in water: Semisynthesis of sophocarpine
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A metal-free, environment friendly, easy-to-operate, and efficient method for the semisynthesis of sophocarpine from matrine has been developed in an overall yield of 91%. The route features a controllable and efficient oxidation of thioether to sulfoxide by 2-iodoxybenzoic acid (IBX) in water.
- Li, Chaojie,Liu, Yuxiu,Wang, Qingmin
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p. 950 - 953
(2015/02/19)
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- A study of the structure of albertine
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Albertine, isolated from the epigeal part of Leontice albertii, is the first hydroxyl-containing unsaturated alkaloid of the matrine series. On the basis of a study of its mass and NMR spectra and its conversion into sophoramine and matridine, its structure has been established as 13e-hydroxy-7,11-dehydromatrine.
- Iskandarov,Kamalitdinov,Yunusov
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p. 596 - 598
(2007/10/09)
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