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Part-IIIAdvances Dihydropyridines and …[(S)] is the biologically active enantiomer, indicating a more potent and specific Eg5inhibitor.OHOONHNHMonastrol 117Although many reports have been dedicated to elucidate the mechanism of action ofmonastrol as mitotic inhibitor in the cell cycle, 180-182Sfew examples concerning theanticancer activity 183-186 were reported. Recently, Leizerman and coworkers described thedifferential effects of monastrol on AGS and HT-29 cell lines in comparison with taxol. 187Further, Russowsky et al., 188 investigated firstly the differential anti-proliferative activityof monastrol 117 and its oxo-analogue, named oxo-monastrol 118, as well as the thioanalogues119a-123a and the corresponding oxo-analogues 119b-123b (all compounds inthe racemic form) on seven human cancer cell lines.Monastrol and the thio-derivatives 120a, 121a and 123a displayed relevantantiproliferative properties with 3,4-methylenedioxy derivative 123a being approximatelymore than 3 times more potent than monastrol against colon cancer (HT-29) cell line.437

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