74519-03-2Relevant academic research and scientific papers
Synthesis and evaluation of stilbenylbenzoxazole and stilbenylbenzothiazole derivatives for detecting β-amyloid fibrils
Lee, Ji Hoon,Byeon, Seong Rim,Lim, Soo Jeong,Oh, Seung Jun,Moon, Dae Hyuk,Yoo, Kyung Ho,Chung, Bong Young,Kim, Dong Jin
, p. 1534 - 1537 (2008/12/20)
This paper describes a novel series of stilbenylbenzoxazole (SBO) and stilbenylbenzothiazole (SBT) derivatives for β-amyloid specific binding probes. These 24 compounds were synthesized and evaluated by competitive binding assay against β-amyloid 1-42 (Aβ42) aggregates using [125I]TZDM. All the derivatives displayed higher binding affinities with Ki value in the subnanomolar range (0.10-0.74 nM) than Pittsburgh Compound-B (PIB) (0.77 nM). Among these derivatives, SBT-2, 5-fluoroethoxy-2-{4-[2-(4-methylaminophenyl)vinyl]phenyl}benzothiazole, showed lowest Ki value (0.10 nM). In conclusion, the preliminary results suggest that these compounds are implying a possibility as a probe for detection of Aβ fibrils in Alzheimer's disease (AD) patients.
Metabolic N-Hydroxylation. Use of Substituent Variation to Modulate the in Vitro Bioactivation of 4-Acetamidostilbenes
Hanna, Patrick E.,Gammans, Richard E.,Sehon, Russell D.,Lee, Man-Kil
, p. 1038 - 1044 (2007/10/02)
N-Hydroxylation is an obligate step in the bioactivation of carcinogenic aryl amides.Previous reports from this laboratory demonstrated that variation of the 4' substituent of trans-4-acetamidostilbene (1) has a marked effect on the rate of its in vitro m
