6628-97-3Relevant articles and documents
Copper-catalyzed one-pot amine-alkylation of quinones with amines and alkanes
Yang, Jian,Wang, Bei,Zhang, Yuankang,Zhang, Shuqing,He, Shuai,Shi, Zhi-Chuan,Wang, Ji-Yu
, p. 988 - 992 (2021)
A copper-catalyzed one-pot amine-alkylation of quinones with amines and alkanes in the presence of di-tert-butyl peroxide (DTBP) was developedviaa radical reaction process. Various alkanes and aromatic or aliphatic amines with diverse structures and electronic properties are suitable substrates, and the chirality of amines can be maintained for the transformation. This method has high step and atom economy for straightforward access to aminated and alkylated quinones from readily available starting materials.
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.
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.
