464920-03-4Relevant academic research and scientific papers
HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues
Xia, Yan,Jin, Yinglan,Kaur, Navneet,Choi, Yongseok,Lee, Kyeong
experimental part, p. 2386 - 2396 (2011/06/21)
The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
Synthesis of the F11334's from o-prenylated phenols: ΜM inhibitors of neutral sphingomyelinase (N-SMase)
Lindsey, Christopher C,Gómez-Díaz, Consuelo,Villalba, José M,Pettus, Thomas R.R
, p. 4559 - 4565 (2007/10/03)
F11334A1, F11334A2, F11334A3, and their corresponding resorcinol analogs were synthesized along with F11334B1, and F11263. In the course of these synthetic studies, several conditions for manipulating (2,3-propanediol) and (2,3-epoxypropyl) o-substituted phenols were developed as well as a variety of conditions for cleavage of aryl O-t-butyl carbonates. From enzyme assays it appears that the hydroquinone nucleus is the essential structural necessary for N-SMase inhibition. Furthermore, it appears that this family of compounds is comprised of irreversible inhibitors.
