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Design, Synthesis and Biological Evaluations of a Novel Series of Enediynes Constituted with DNA Cleavage, Alkylating and DNA Binding Agents via Varies Spacers
Author(s) -
Lin ChiFong,
Hwang Martin,
Kuo YaoHaur,
Wu MingJung
Publication year - 2007
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.200700074
Subject(s) - chemistry , hela , cleavage (geology) , dna , stereochemistry , cytotoxic t cell , nucleic acid , dna supercoil , microbiology and biotechnology , cell , biochemistry , in vitro , dna replication , geotechnical engineering , fracture (geology) , biology , engineering
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 IC 50 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.