64505-52-8Relevant articles and documents
Computer-aided design of 1,4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases
Cardoso, Sílvia Helena,Guimar?es, Ari Souza,McKerrow, James H.,Silva, Leandro Rocha,da Silva, Elany Barbosa,da Silva-Júnior, Edeildo Ferreira,do Nascimento, Jadiely,do Santos Nascimento, Igor José
, (2021/05/21)
Chagas disease and Human African Trypanosomiasis (HAT) are caused by Trypanosoma cruzi and T. brucei parasites, respectively. Cruzain (CRZ) and Rhodesain (RhD) are cysteine proteases that share 70% of identity and play vital functions in these parasites.
Exploration of Benzo[b]carbazole-6,11-diones as anticancer agents: Synthesis and studies of hTopoIIα inhibition and apoptotic effects
Banerjee, Uttam C.,Chaudhary, Hiteshkumar,Daniel, Divine P,Das, Biswajit,Grewal, Preeti,Guchhait, Sankar K.,Kumar, Gulshan,Kundu, Chanakya N.,Nayak, Deepika,Paul, Subarno,Sisodiya, Shailendra
supporting information, (2021/08/12)
Two series of (hetero)arylamino-naphthoquinones and benzo-fused carbazolequinones were considered for study with the rationale that related structural motifs are present in numerous drugs, clinical trial agents, natural products and hTopoIIα inhibitors. Total 42 compounds were synthesized by reactions including dehydrogenative C–N and Pd-catalyzed C–C bond forming transformations. These compounds were screened against numerous cancer cells including highly metastatic one (MCF-7, MDA-MB-231, H-357 and HEK293T), and normal cells (MCF 10A). Some of the active compounds were evaluated for clonogenic cell survival and apoptotic effects in cancer cells (DAPI nuclear staining, Comet assay, Annexin-V-FITC/PI dual staining, flow cytometry, and western blot analysis with relevant proteins). All compounds were tested for hTopoIIα inhibitory activity. The investigated series compounds showed important properties like significant apoptotic antiproliferation in cancer cells with cell cycle arrest at S-phase and downregulation of NF- κβ signaling cascade, relatively less cytotoxicity to normal cells, and hTopoIIα inhibition with more efficiency compared to an anticancer drug etoposide.
Method for synthesizing 2-substituted amino-1,4-naphthoquinone derivative
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Paragraph 0044-0049, (2019/05/28)
The invention discloses a method for synthesizing a 2-substituted amino-1,4-naphthoquinone derivative. The method comprises the following steps: mixing a nitro compound, 2-substituted 1,4-naphthoquinone, a catalyst, a metal and a solvent uniformly at 20-100 DEG C; adding an H source, stirring the components for reaction for 1-24h; performing a reduction-addition reaction between the nitro compoundand the 2-substituted 1,4-naphthoquinone; after the reaction, adding water to the reaction system for dilution; performing filtering; extracting filtrate with ethyl acetate; after organic phases arecombined, washing the mixture with saturated saline solution and drying the mixture with anhydrous sodium sulfate sequentially; subsequently, performing filtering, and performing vacuum concentrationto remove a solvent; and packing solids into a column, and performing separation through column chromatography (a ratio of petroleum ether to ethyl acetate is 5:1) to obtain red solids. Compared withan existing synthesis method, the synthesis method provided by the invention has a wide range of raw materials and the raw materials are easy to obtain; compared with amine compounds, nitro compoundshave better stability; and the synthesis method provided by the invention is simple to operate and mild in reaction condition.
