1632-49-1Relevant academic research and scientific papers
Structure-activity relationships study of neolamellarin A and its analogues as hypoxia inducible factor-1 (HIF-1) inhibitors
Li, Guangzhe,Dong, Huijuan,Ma, Yao,Shao, Kun,Li, Yueqing,Wu, Xiaodan,Wang, Shisheng,Shao,Zhao, Weijie
supporting information, p. 2327 - 2331 (2019/07/09)
The novel marine pyrrole alkaloid neolamellarin A derived from sponge has been shown to inhibit hypoxia-induced HIF-1 activity. In this work, we designed and synthesized neolamellarin A and its series of derivatives by a convergent synthetic strategy. The HIF-1 inhibitory activity and cytotoxicity of these compounds were evaluated in Hela cells by dual-luciferase reporter gene assay and MTT assay, respectively. The results showed that neolamellarin A 1 (IC50 = 10.8 ± 1.0 μM) and derivative 2b (IC50 = 11.9 ± 3.6 μM) had the best HIF-1 inhibitory activity and low cytotoxicity. Our SAR research focused on the effects of key regions aliphatic carbon chain length, aromatic ring substituents and C-7 substituent on biological activity, providing a basis for the subsequent research on the development of novel pyrrole alkaloids as HIF-1 inhibitors and design of small molecule probes for target protein identification.
Synthetic hosts for molecular recognition of ureas
Maria, Dolores Santa,Farran, M. Angeles,Garcia, M. Angeles,Pinilla, Elena,Torres, M. Rosario,Elguero, Jose,Claramunt, Rosa M.
experimental part, p. 6780 - 6788 (2011/10/18)
Four hosts (7-10) containing 2,6-bisamidopyridine- and 2,5-bisamidopyrrole- bearing pyridyl or 1,8-naphthyridyl groups have been prepared and their structures studied by a combination of multinuclear NMR spectroscopy and X-ray crystallography. Their behav
Synthesis of 1',2',3',4',5'-pentamethyl-3,4-diphenylazaferrocene and its enantioselective C-2 functionalization via (-)-sparteine-mediated lithiation
Fukuda, Tsutomu,Koga, Yasuyuki,Iwao, Masatomo
experimental part, p. 1237 - 1248 (2009/06/28)
Lithiation of 1',2',3',4',5'-pentamethyl-3,4-diphenylazaferrocene (9) with sec-BuLi/(-)-sparteine (2) in Et2O at -78 °C followed by quenching with electrophiles gave the C-2 functionalized azaferrocenes (17) in good enantioselectivities (up to
