- Synthesis and biological evaluation of vanadium complexes as novel anti-tumor agents
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A class of vanadium complexes were prepared and investigated for their antiproliferative effects by MTT assay. The structure-activity relationship was extensively studied through the ligand variation. The results showed that the synthetic vanadium complexes demonstrated moderate to good antiproliferative activities against the four cancer cell lines including MGC803, EC109, MCF7 and HepG2, respectively. Of note was that most of the complexes showed preferential growth inhibitory activity to some degree toward gastric cancer line MGC803. Among them, complex 19 exhibited the most and broad-spectrum proliferative inhibition against the tested cell lines. In addition, mechanism studies illustrated that complex 19 could prevent the colony formation, migration and EMT process, as well as induce apoptosis of MGC803 cells. Furthermore, Western blot experiments revealed that the expression of apoptosis-related proteins changed, including up-regulation of Bax, PARP and caspase-3/9, as well as down-regulation of Bcl-2.
- Lu, Ling-Pan,Suo, Feng-Zhi,Feng, Ya-Li,Song, Li-Li,Li, Ying,Li, Yang-Jie,Wang, Kai-Ti
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- Evolution of a Strategy for the Enantioselective Total Synthesis of (+)-Psiguadial B
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(+)-Psiguadial B is a diformyl phloroglucinol meroterpenoid that exhibits antiproliferative activity against the HepG2 human hepatoma cancer cell line. This full account details the evolution of a strategy that culminated in the first enantioselective total synthesis of (+)-psiguadial B. A key feature of the synthesis is the construction of the trans-cyclobutane motif by a Wolff rearrangement with in situ catalytic, asymmetric trapping of the ketene. An investigation of the substrate scope of this method to prepare enantioenriched 8-aminoquinolinamides is disclosed. Three routes toward (+)-psiguadial B were evaluated that featured the following key steps: (1) an ortho-quinone methide hetero-Diels-Alder cycloaddition to prepare the chroman framework, (2) a Prins cyclization to form the bridging bicyclo[4.3.1]decane system, and (3) a modified Norrish-Yang cyclization to generate the chroman. Ultimately, the successful strategy employed a ring-closing metathesis to form the seven-membered ring and an intramolecular O-arylation reaction to complete the polycyclic framework of the natural product.
- Chapman, Lauren M.,Beck, Jordan C.,Lacker, Caitlin R.,Wu, Linglin,Reisman, Sarah E.
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p. 6066 - 6085
(2018/05/15)
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- Accessible, highly active single-component β-ketiminato neutral nickel(II) catalysts for ethylene polymerization
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A series of novel neutral nickel complexes based on cyclic β-ketiminato ligands, [(2,6-iPr2C6H 3)N - CHC6H8O]Ni(Ph)(PPh3) (3b), [(2,6-iPr2C6H3)N - CHC n+3H2n+2O(C6H4)]Ni(Ph)(PPh 3) (6a-c), and [(2,6-iPr2C6H 3)N - CHCn+3H2n+2O(C6H 4)]Ni(CH3)(Py) (7a-c: a, n = 0; b, n = 1; c, n = 2) have been synthesized and characterized. These conveniently accessible complexes proved to be highly active catalysts for ethylene polymerization without an activator. Under the optimized conditions, an activity of 71.4 kg of PE/((mol of Ni) h atm) was observed using 6c as a catalyst. Particularly, it is of great interest that a bulky substituent proximate to the oxygen atom of the β-ketiminato complex is no longer a prerequisite to attain high catalytic efficiency, which is much different from the case for salicylaldiminato neutral nickel catalysts. This is effectively supported by the lower activation enthalpy changes of complexes 3b and 6a-c relative to values for the classic salicylaldiminato complexes. Moreover, for complexes 6a-c and 7a-c, the degree of conjugation between the phenylene ring and the corresponding nickel chelate of the complex can be tuned via changes in the ligand structure, which remarkably influence the molecular weights and the microstructures of the resulting polyethylenes. In comparison with the highly conjugated complexes 6a and 7a, complexes 6b,c and 7b,c, with a low degree of conjugation, produced polyethylenes with much higher molecular weights and lower branch contents. X-ray crystallographic analysis of 3b and 6a-c provides detailed information about the differences among these structures, and various typical angles and bond distances produce evidence of the conjugation modulation effect.
- Song, Dong-Po,Wu, Ji-Qian,Ye, Wei-Ping,Mu, Hong-Liang,Li, Yue-Sheng
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experimental part
p. 2306 - 2314
(2010/07/04)
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