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Title: Synthesis and biological evaluation of isoindigo derivatives as anti-proliferative agents
Authors: WEE XI KAI
Keywords: Meisoindigo, isoindigo, chronic myelogenous leukemia, antiproliferative, anti-cancer, lead optimization
Issue Date: 4-Aug-2011
Citation: WEE XI KAI (2011-08-04). Synthesis and biological evaluation of isoindigo derivatives as anti-proliferative agents. ScholarBank@NUS Repository.
Abstract: Meisoindigo has been utilized as a Chinese medication for chronic myleogenous leukemia (CML) for many years. This project aims to utilize meisoindigo as a lead to design and synthesize functionalized isoindigos with enhanced potency and pharmaceutically friendly profiles. 93 synthesized isoindigo analogues were evaluated for growth inhibitory activities on a chronic myelogenous leukemia cell line (K562). Of these, D5 was observed to have the best anti-proliferative activity which is significantly better than meisoindigo. Despite having promising selectivity profiles and inhibited cell cycle at G2 phase, D5 is hampered by its poor aqueous solubility. In spite of its potent in vitro activity, D5 failed to extend survival times of the xenograft bearing mice or significantly reduced the tumour volume in vivo. In contrast, F4 was observed to have excellent solubility with better in vitro activity than meisoindigo and resulted in significant improvements in both survival times and tumor size in vivo.
Appears in Collections:Ph.D Theses (Open)

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