• 약학회지
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• 제45권4호
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• pp.321-327
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• 2001

The synthesis of novel taxol analogues with an amine moiety at the 7- and 10-positions to examine the BBB penetration was described. The analogues were synthesized from 2'-O-(tert-butyldim-ethylsilyl)taxol and 2'-0-(tert-butyldimethylsilyl) -7-O-(triethylsilyl)-10-deacetyltaxol, the key intermediates, in 2 steps via the esterification with heterocyclic amino acids and the subsequent desilylation reaction.

• Asian Pacific Journal of Cancer Prevention
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• 제13권2호
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• pp.563-567
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• 2012

In our era there has been several anti-cancer drugs which have undergone both experimental and clinical trials; however, due to their poor solubilities, numerous side effects, insufficient bioavailability and poor compliance, many have resulted into poor outcomes. Therefore, our aim was to investigate the effects of novel hydrophilic taxanes analogues CQMU-0517 and CQMU-0519 on growth of A549 lung, SKVO3 ovary and MCF7 breast carcinoma cell lines. Different concentrations of original paclitaxel, CQMU-0517, original docetaxel and CQMU-0519 were utilized on three cell lines, where cell growth was assessed using cell culture kit-8 and flow cytometry analysis. The results unveiled that CQMU-0517 and CQMU-0519 suppressed cell growth in the three particular cell lines, cell cycle arrest being evident in the G2/M phase. Hence, the results showed that these new taxane analogues have potential and warrant future clinical trials.