Design,Synthesis and Biological Evaluations of a Novel Series of Enediynes Constituted with DNA Cleavage,Alkylating and DNA Binding Agents via Varies Spacers |
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| Authors: | Chi‐Fong Lin Martin Hwang Yao‐Haur Kuo Ming‐Jung Wu |
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| Institution: | 1. Department of Biological Science and Technology, Chung Hwa College of Medical Technology, Tainan, Taiwan, R.O.C.;2. Faculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan, R.O.C.;3. National Research Institute of Chinese Medicine, Taipei, Taiwan, R.O.C. |
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| Abstract: | Among the three series of complicated combinatory enediynes, 3a?d were more active than 2a?c and 4a?b , in which 3a?b showed equally inhibitory activity against the growth of Hepa59T/VGH, KB and Hela with mean IC50 values lower than 10 μg/mL. Compounds 2a and 3b exhibited the most potent inhibitory activity against the growth of Hela cells for 4.39 μg/mL. Derivative 3d displayed the greatest ability against the growth of Hepa59T/VGH cell lines for 6.95 μg/mL, while 3a showed more cytotoxic to KB cells than other analogs. Conjugates 2a‐c presented better responses than 3a‐d for the DNA cleavage assay of supercoiled ΦX174. |
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| Keywords: | Enediyne Antitumor Propargyl sulfone |
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