482288-61-9

Upstream product

• 162705-13-7 (Z)-1-(4''-methoxy-3''-nitrophenyl)-2-(3',4',5'-trimethoxyphenyl)ethene 
• 206649-07-2 (E)-1-(4-methoxy-3-nitrophenyl)-2-(3',4',5'-trimethoxyphenyl)ethene 
• 31680-08-7 4-methoxy-3-nitrobenzaldehyde 
• 61240-20-8 triphenyl-(3,4,5-trimethoxybenzyl)phosphonium bromide 

Relevant academic research and scientific papers

Combretastatin A-4 and Derivatives: Potential Fungicides Targeting Fungal Tubulin

Combretastatin A-4, first isolated from the African willow tree Combretum caffrum, is a tubulin polymerization inhibitor in medicine. It was first postulated as a potential fungicide targeting fungal tubulin for plant disease control in this study. Combretastatin A-4 and its derivatives were synthesized and tested against Rhizoctonia solani and Pyricularia oryzae. Several compounds have EC50 values similar to or better than that of isoprothiolane, which is widely used for rice disease control. Structure-activity relationship study indicated the the cis configuration and hydroxyl group in combretastatin A-4 are crucial to the antifungal effect. Molecular modeling indicated the binding sites of combretastatin A-4 and carbendazim on fungal tubulin are totally different. The bioactivity of combretastatin A-4 and its derivatives against carbendazim-resistant strains was demonstrated in this study. The results provide a new approach for fungicide discovery and fungicide resistance management.

Orchid heterocyclic derivative as well as preparation method and application thereof

The invention relates to a lansamine heterocyclic derivative as well as a preparation method and application thereof. Wherein, X is O or NH. R Is one of a furanyl heterocyclic substituent, a thiophenyl heterocyclic substituent, a thiazolyl heterocyclic substituent, a pyrimidinyl heterocyclic substituent, a pyridazinyl heterocycle substituent, an indolyl heterocyclic substituent, and an indolyl heterocyclic substituent. The preparation method comprises the following steps: carrying out condensation reaction on crude orchid and a carboxylic acid compound containing the substituent R. Or, 4 - methoxy -3 - nitrobenzaldehyde and 3,trimethoxy - triphenyl benzyl bromide salt is used as a raw material, and after Wittig reaction and reduction reaction, the tetracarboxylic acid compound containing the substituent R is subjected to a condensation reaction. Compared with the prior art, heterocyclic compounds such as crude orchid and nicotinic acid are connected through an ester bond to form a twin medicine, and a new way is provided for improving the pharmacological activity of the crude orchid.

5-FLUOROURACIL DERIVATIVES, PREPARATION METHODS AND USES THEREOF

Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.

Preparation and application for 5-fluorouracil substituted carboxylic acid derivative

The invention discloses a preparation and an application for a compound compounded from stilbene and diphenylethane antitumor drugs and 5-fluorouracil antitumor drugs. The compound provided by the invention has a general structural formula (I) as describe

Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs

Abstract A total of 11 novel combretastatin A-4 (CA-4) analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes: (i) hydrogenated derivatives, (ii) ethoxyl derivatives, (iii) amino derivatives and (iv) pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure-activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.

METHOD FOR PRODUCING AMINOSTILBENE DERIVATIVE

Industrial production is conveniently practiced with high efficiency for various specific aminostilbene derivatives or salt(s) thereof such as (Z)-3,4,4',5-tetramethoxy-3'-aminostilbene and the like, which are important as an active component of anticance