1569293-99-7Relevant academic research and scientific papers
Synthesis of 3,4-Fused Tricyclic Indoles through Cascade Carbopalladation and C-H Amination: Development and Total Synthesis of Rucaparib
Cheng, Cang,Zuo, Xiang,Tu, Dongdong,Wan, Bin,Zhang, Yanghui
, p. 4985 - 4989 (2020)
3,4-Fused tricyclic indole scaffolds are ubiquitous in bioactive natural products and pharmaceuticals. A new protocol for the synthesis of 3,4-fused tricyclic indoles has been developed through cascade carbopalladation and C-H amination with N,N-di-tert-butyldiaziridinone. The protocol allows access to a range of 3,4-fused tricyclic indoles, including those containing various linkers and fused with medium-sized rings. Rucaparib can be synthesized via this reaction, providing an advantageous synthetic method for the FDA-approved cancer medicine.
Synthesis and biological evaluation of new quinoxaline derivatives of ICF01012 as melanoma-targeting probes
El Aissi, Radhia,Liu, Jianrong,Besse, Sophie,Canitrot, Damien,Chavignon, Olivier,Chezal, Jean-Michel,Miot-Noirault, Elisabeth,Moreau, Emmanuel
supporting information, p. 468 - 473 (2014/06/09)
The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [ 125I]1a-g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43-5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound 1d will be used as building block for the design of new melanoma-selective drug delivery systems.
