39755-95-8Relevant articles and documents
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy
Chen, Juncheng,Chiang, Cheng-Ming,He, Gu,Liu, Bo,Liu, Jie,Ouyang, Liang,Tang, Pan,Wang, Guan,Yang, Chengcan,Ye, Tinghong,Zhang, Jifa,Zhang, Jin,Zou, Ling
, p. 18025 - 18053 (2022/01/03)
Bromodomain-containing protein 4 (BRD4) is an attractive epigenetic target in human cancers. Inhibiting the phosphorylation of BRD4 by casein kinase 2 (CK2) is a potential strategy to overcome drug resistance in cancer therapy. The present study describes the synthesis of multiple BRD4–CK2 dual inhibitors based on rational drug design, structure–activity relationship, and in vitro and in vivo evaluations, and 44e was identified to possess potent and balanced activities against BRD4 (IC50 = 180 nM) and CK2 (IC50 = 230 nM). In vitro experiments show that 44e could inhibit the proliferation and induce apoptosis and autophagy-associated cell death of MDA-MB-231 and MDA-MB-468 cells. In two in vivo xenograft mouse models, 44e displays potent anticancer activity without obvious toxicities. Taken together, we successfully synthesized the first highly effective BRD4–CK2 dual inhibitor, which is expected to be an attractive therapeutic strategy for triple-negative breast cancer (TNBC).
Metal-free synthesis of benzimidazo[1,2-c]quinazolin-6-ones with indole and benzenediamine oxidized by I2/TBHP
Dai, Zhen,Li, Songhua,Li, Yunyi,Feng, Lei,Ma, Chen
supporting information, p. 2012 - 2017 (2019/02/20)
A variety of benzimidazo[1,2-c]quinazolin-6-ones derivatives can be accessed in moderate to good yields under simple and metal-free reaction conditions using indoles and o-benzenediamines oxidized by iodine and TBHP. This procedure works in reasonable yields for different indoles as well as o-benzenediamines thus may provide a good synthesis of quinazolinones. A TBHP oxidized ring expansion reaction mechanism that explains the synthesis of benzimidazo[1,2-c]quinazolin-6-ones were reported.
An efficient synthesis of versatile synthon 3-chlorooxindoles with NaCl/oxone
Lakshmi Reddy, Vanammoole,Prathima, Parvathaneni Sai,Rao, Vaidya Jayathirtha,Bikshapathi, Raktani
, p. 20152 - 20155 (2018/12/13)
The present work describes an expedient approach for the direct conversion of indole-3-carboxaldehyde to 3-chlorooxindoles using a simple sustainable synthetic method. From an environmental perspective, a combination of NaCl/oxone in a CH3CN?:?H2O (1?:?1) system was developed for direct oxidative chlorination of a wide array of indole derivatives. This chlorination strategy is more viable, remarkably cheaper and provides easy access to potential 3-chlorooxindoles. In addition, this environmentally benign method can also be applicable for constructing isatin derivatives in good yields.
