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We report on the solid‐phase synthesis of a combinatorial methylated (±)‐epigallocatechin gallate (EGCG) library and its biological evaluation. Epigallocatechin gallate (EGCG) and its methylated derivatives, which are members of the catechin family, exhibit various anti‐cancer effects. The solid‐phase synthesis of methylated EGCG involves the preparation of the α‐acyloxyketone by the coupling of a solid‐supported aldehyde with a ketone and an acid. The subsequent release and reductive etherification reaction of the solid‐supported α‐acyloxyketone provide the protected EGCG in good total yields. Sixty‐four methylated EGCGs were successfully prepared. The growth‐inhibitory effects of the methylated EGCG library were also examined. Although methylation of EGCG generally causes reduced growth inhibition, the growth‐inhibitory effect of 7‐OMe EGCGs was comparable to that of EGCG. The 7‐OMe EGCGs are attractive drug candidates because of their enhanced bioavailability.A brand new combine harvester: The solid‐phase synthesis of a combinatorial methylated (±)‐epigallocatechin gallate (EGCG) library is reported. Deprotection of the protected EGCG is achieved by utilizing a continuous‐flow hydrogenation reactor (H‐Cube). The growth‐inhibitory effects of the methylated EGCG library reveal that 7‐OMe EGCGs exhibit comparable biological activity to natural EGCG.
| Authors: | Tanaka, Hiroshi; Yamanouchi, Maasa; Miyoshi, Haruko; Hirotsu, Keisuke; Tachibana, Hirofumi; Takahashi, Takashi | |
| Journal: | Chemistry - An Asian Journal | |
| Volume: | 5 | |
| edition: | 10 | |
| Year: | 2010 | |
| Pages: | 2231 | |
| DOI: | 10.1002/asia.201000372 | |
| Publication date: | 04-Oct-2010 |
The unfolding landscape of the congenital myasthenic syndromes
Abstract Congenital myasthenic syndromes (CMS) are heterogeneous disorders in which the safety margin of neuromuscular transmission is impaired by one or more specific mechanisms. Since the advent of next‐generation sequencing methods, the discovery of novel CMS targets and phenotypes ha ... more
Passive transfer models of myasthenia gravis with muscle‐specific kinase antibodies
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Abstract Because of the failure of many promising therapeutics identified in preclinical evaluation, funding sources have established guidelines for increased rigor in animal evaluations. The myasthenia gravis (MG) community of scientists has developed guidelines for preclinical assessme ... more
Smart skin made of recyclable materials may transform medicine and robotics
Smart skin that can respond to external stimuli could have important applications in medicine and robotics. Using only items found in a typical household, researchers have created multi-sensor artificial skin that's capable of sensing pressure, temperature, humidity, proximity, pH, and air ... more
How mercury contamination affects reptiles in the Amazon basin
Mercury contamination in water and on land is of worldwide concern due to its toxic effects on ecosystems and human health. Mercury toxicity is of particular concern to reptiles because they are currently experiencing population declines. Also, reptiles are ideal indicators of mercury conta ... more
Bioengineers Succeed in Producing Plastic Without the use of Fossil Fuels
A team of pioneering South Korean scientists have succeeded in producing the polymers used for everyday plastics through bioengineering, rather than through the use of fossil fuel based chemicals. This groundbreaking research, which may now allow for the production of environmentally consci ... more
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