Six active compounds are isolated from the marine bryozoan Bugula neritina,inhabiting the Nanwan Bay in the South China Sea, using the bioassay-guided method with a combination of extraction and partitionation with su...Six active compounds are isolated from the marine bryozoan Bugula neritina,inhabiting the Nanwan Bay in the South China Sea, using the bioassay-guided method with a combination of extraction and partitionation with suitable solvents as well as multiple column chromatographies ( Sephadex LH-20, ODS and preparative HPLC).Their structures are identified as known bryostatins-bryostatins 4, 5, 6, 10, 11 and 18 through intensive analysis of the data of high resolution 2D NMR (600 MHz, DQF-COSY,TOCSY, HMQC and ROESY) and ESI-MS. Among them, bryostatins 10, 11 and 18 are for the first time obtained from this bryozoan in the South China Sea and they show significant antineoplastic activities in vitro.展开更多
A convergent approach to 1,5-hydroxy ketones,the general precursors for constructing the C ring of bryostatins,has been developed via a Zn/Cu-promoted conjugate addition of a-hydroxy iodides with enones.The reaction l...A convergent approach to 1,5-hydroxy ketones,the general precursors for constructing the C ring of bryostatins,has been developed via a Zn/Cu-promoted conjugate addition of a-hydroxy iodides with enones.The reaction leads to direct formation of the C21-C22 bond and tolerates diverse functionalities at the C17-,C18-and C24-positions.The approach also enables a more concise synthesis of the known C ring intermediate(10 longest linear steps and 14 total steps),in contrast to its previous synthesis(17 longest linear steps and 22 total steps) in our total synthesis of bryostatin 8.展开更多
基金the National Natural Science Foundation of China(NNSFC,29672050).
文摘Six active compounds are isolated from the marine bryozoan Bugula neritina,inhabiting the Nanwan Bay in the South China Sea, using the bioassay-guided method with a combination of extraction and partitionation with suitable solvents as well as multiple column chromatographies ( Sephadex LH-20, ODS and preparative HPLC).Their structures are identified as known bryostatins-bryostatins 4, 5, 6, 10, 11 and 18 through intensive analysis of the data of high resolution 2D NMR (600 MHz, DQF-COSY,TOCSY, HMQC and ROESY) and ESI-MS. Among them, bryostatins 10, 11 and 18 are for the first time obtained from this bryozoan in the South China Sea and they show significant antineoplastic activities in vitro.
基金the financial support from the National Natural Science Foundation of China(No.21921002)the NationalScience and Technology Major Project of the Ministry of Science and Technology of the People’s Republic of China(No.2018ZX09711001-005-004)the Fundamental Research Funds for the Central Universities(No.2012017yjsy210)。
文摘A convergent approach to 1,5-hydroxy ketones,the general precursors for constructing the C ring of bryostatins,has been developed via a Zn/Cu-promoted conjugate addition of a-hydroxy iodides with enones.The reaction leads to direct formation of the C21-C22 bond and tolerates diverse functionalities at the C17-,C18-and C24-positions.The approach also enables a more concise synthesis of the known C ring intermediate(10 longest linear steps and 14 total steps),in contrast to its previous synthesis(17 longest linear steps and 22 total steps) in our total synthesis of bryostatin 8.
