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Mimicry of Annonaceous Acetogenins: Enantioselective Synthesis of a (4R)-Hydroxy Analogue Having Potent Antitumor Activity
journal contribution
posted on 2002-04-20, 00:00 authored by Sheng Jiang, Zhong-Hai Liu, Gang Sheng, Bu-Bing Zeng, Xiao-Guang Cheng, Yu-Lin Wu, Zhu-Jun YaoThe (4R)-hydroxylated analogues of annonaceous acetogenin mimicking compound 2 were designed
and synthesized structurally on the basis of the naturally occurring annonaceous acetogenin
bullatacin, which was discovered as a typical member of the novel family of polyketides with potent
cytotoxicity, antitumoral, and other biological activities. The preliminary screenings show that the
IC50 values of 2 were 1.6 × 10-3 and 8 × 10-2 μg/mL against HT-29 and HCT-8, respectively. A
remarkable enhancement effect was observed by the activity comparison of 1c and its (4R)-hydroxylated analogue 2.
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AnnonaceouEnantioselective1 c1.6HTcompound 2activity comparisonanalogueMimicryhydroxylatedenhancement effectbasispolyketidenovel familyantitumoralmemberscreenings showIC 50 valuesSynthesiHCTAcetogeninannonaceous acetogeninHydroxycytotoxicityPotent Antitumor ActivityAnalogueannonaceous acetogenin bullatacin
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