An
125I-labeled resveratrol derivative 1 was synthesized. It was purified by reverse phase HPLC. Radiochemical purity of the product was more than 98%, and the yield was 35% (decay-corrected). Its biodistribution in tumorbearing mice was studied. The results showed that the highest radioactivity was located in intestine and stomach. The biodistribution profile suggests that compound 1 can be effectively used as a promising imaging probe for intestine and stomach.
Design, Synthesis, and Antiproliferative Activity of New 1H-Pyrrolo[3,2-c]pyridine Derivatives Against Melanoma Cell Lines. -Diarylureas and diarylamides having a pyrrolopyridine scaffold are synthesized involving a nucleophilic displacement of the 4-chloro group of azaindole (I) by the aromatic amino group and a subsequent rearrangement of the resulting secondary amine to afford the key intermediates (III). The new compounds generally inhibit the growth of A375P human melanoma cell line with superior activity compared to the reference standard. Some compounds also reveal superior selectivity towards melanoma cells than NIH3T3 fibroblasts. The most potent compounds, diarylamide (VId) and diarylurea (XI), are further tested over nine melanoma cell lines. Both compounds demonstrate high potency. -(EL-GAMAL, M. I.; JUNG, M.-H.; LEE, W. S.; SIM, T.; YOO, K. H.; OH*, C.-H.; Eur. J. Med. Chem. 46 (2011) 8, 3218-3226, http://dx.
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