1325214-49-0Relevant articles and documents
Indenone derivatives as inhibitor of human DNA dealkylation repair enzyme AlkBH3
Nigam, Richa,Babu, Kaki Raveendra,Ghosh, Topi,Kumari, Bhavini,Akula, Deepa,Rath, Subha Narayan,Das, Prolay,Anindya, Roy,Khan, Faiz Ahmed
, p. 4100 - 4112 (2018)
The mammalian AlkB homologue-3 (AlkBH3) is a member of the dioxygenase family of enzymes that in humans is involved in DNA dealkylation repair. Because of its role in promoting tumor cell proliferation and metastasis of cancer, extensive efforts are being directed in developing selective inhibitors for AlkBH3. Here we report synthesis, screening and evaluation of panel of arylated indenone derivatives as new class of inhibitors of AlkBH3 DNA repair activity. An efficient synthesis of 2,3-diaryl indenones from 2,3-dibromo indenones was achieved via Suzuki-Miyaura cross-coupling. Using a robust quantitative assay, we have obtained an AlkBH3 inhibitor that display specific binding and competitive mode of inhibition against DNA substrate. Finally, we established that this compound could prevent the proliferation of lung cancer cell line and enhance sensitivity to DNA damaging alkylating agent.
Synthesis of indenones through rhodium(III)-catalyzed [3+2] annulation utilizing a recyclable carbazolyl leaving group
Ochiai, Shiho,Sakai, Asumi,Usuki, Yoshinosuke,Kang, Bubwoong,Shinada, Tetsuro,Satoh, Tetsuya
, (2021/04/23)
The rhodium(III)-catalyzed annulative coupling of 9-ben-zoylcarbazoles with internal alkynes proceeds efficiently through ortho CH and CN bond cleavages. This reaction provides direct access to variously substituted indanone derivatives. The carbazolyl leaving group can be readily recovered and reused for preparing the starting materials.
Efficient indenones synthesis via iridium-catalyzed decarboxylative annulation between 2-oxo-2-phenylacetic acids and alkynes
Yu, Xiaobo,Geng, Shudong,Liu, Guanchen,Guo, Weijie,Wang, Jianhui
, p. 139 - 143 (2018/11/23)
Efficient iridium-catalyzed decarboxylative annulation reactions between 2-oxo-2-phenylacetic acids and alkyne derivatives has been achieved. [IrCp*Cl2]2 with a (CH3OC6H4)3P ligand, AgSbF6 and Cu(OAc)2 additives was the most efficient catalytic system for this transformation. This reaction is suitable for a broad range of alkynes and 2-oxo-2-phenylacetic acids and a variety of indenone derivatives were obtained in medium to high yields. This work provides an efficient approach for the construction of indenones by iridium–catalyzed decarboxylative annulation.
