293743-31-4Relevant articles and documents
Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2
Li, Xinyu,Wu, Chengzhe,Lin, Xin,Cai, Xuerong,Liu, Linyi,Luo, Guoshun,You, Qidong,Xiang, Hua
, p. 445 - 455 (2019)
SERMs are a series of important small molecular compounds to modulate estrogen receptor, such as tamoxifen. Although these drugs have showed great benefits in the treatment of breast cancer, the risk of endometrial cancer and endocrine resistance restrict their use. The reasonable designing of multi-target drugs can decrease the side effects and improve the tolerance of antineoplastic agents Studies have identified that VEGFR-2 plays a pivotal role in tumor angiogenesis and drug resistance. Besides, a combination of Tamoxifen and low dose of a VEGFR-2 inhibitor was reported to maximize therapeutic efficacy as well as to retard SERM resistant tumor growth. In this work, a series of 3-aryl-quinolin derivatives were designed to target to ERα and VEGFR-2 to eliminate the disadvantages of SERMs. We identified that compounds 12f and 13f displayed highly ERα binding affinities as well as relative intensity VEGFR-2 inhibitory activities. Moreover, this two compounds exhibited excellent anti-proliferative activities against MCF-7 and HUVEC cell lines with low micromolar IC50 (1–8 μM). A further study confirmed that compound 13f can reduce the expression of PgR mRNA, arrest cell cycle in MCF-7 breast cancer cells, and restrain the cell migration. Overall, based on the biological activities data, 13f can be chosen as a potential anti-cancer lead compound for further studying.
Sulfuryl Fluoride Mediated Synthesis of Amides and Amidines from Ketoximes via Beckmann Rearrangement
Gurjar, Jitendra,Fokin, Valery V.
supporting information, p. 10402 - 10405 (2020/07/25)
A metal-free and redox-neutral method for Beckmann rearrangement employing inexpensive and readily available SO2F2 gas is described. The reported transformation proceeds at ambient temperature and is compatible with a wide range of sterically and electronically diverse aromatic, heteroaromatic, aliphatic and lignin-like oximes providing amides in good to excellent yields. The reaction proceeds through the formation of an imidoyl fluoride intermediate that can also be used for the synthesis of amidines.
Synthesis of α-ketoamides using potassium superoxide (KO2) as an oxidizing agent
Vasudevan,Routholla, Ganesh,Teja Illa, Giri,Reddy, D. Srinivasa
, (2020/05/25)
A simple and convenient method for the synthesis of α-ketoamides by the oxidation of aryl acetamides using potassium superoxide (KO2) as an oxidizing agent is disclosed here. The scope of the developed method is successfully tested with fifteen substrates. In addition, the utility of method has been demonstrated by synthesizing an orexin receptor antagonist, a medicinally interesting compound.