127118-98-3Relevant academic research and scientific papers
(Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine
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, (2019/10/01)
The invention discloses a (Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine. In a general formula (I) shown as the accompanying drawing, Rl is selected from substituted or nonsubstituted saturated nitrogen-containing multivariate heterocycles, substituted or nonsubstituted unsaturated sulfur-containing multivariate heterocycles, and substituted or nonsubstituted unsaturated oxygen containing multivariate heterocycles, and the multivariate heterocycles are 4 to 6 membered heterocycles. R2 is 5-tertiary butyl-1H-imidazole or pyridine. The invention also discloses a purpose of the compound to preparation of medicine composition aspects for treating tumor diseases, particularly, purposes to preparation of medicine compositions for treating pancreatic cancer and/or lung cancer aspects.
Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure
Fu, Zhangyu,Hou, Yingwei,Ji, Cunpeng,Ma, Mingxu,Tian, Zhenhua,Deng, Mengyan,Zhong, Lili,Chu, Yanyan,Li, Wenbao
, p. 2061 - 2072 (2018/03/26)
Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC50 at 1.56 and 1.72 nM, respectively. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization. Furthermore, the interaction between tubulin and these compounds were elucidated by molecular docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe20, which could enhance their binding affinities.
CARBONYLATIVE COUPLING REACTION OF ORGANOFLUOROSILANES WITH ORGANIC HALIDES PROMOTED BY FLUORIDE ION AND PALLADIUM CATALYST
Hatanaka, Yasuo,Fukushima, Satoshi,Hiyama, Tamejiro
, p. 2113 - 2126 (2007/10/02)
Palladium-catalyzed carbonylative cross coupling reaction of organofluorosilanes with organic halides was achieved in the presence of fluoride ion and an atmospheric pressure of carbon monoxide.Alkenyl- or arylfluorosilanes effectively underwent this reaction with alkenyl or aryl iodides in moderate to good yields.Thus, highly functionalized ketones are readily available without protection of reactive functional group such as aldehyde, ketone, ester, nitril, and alcohol.For smooth ketone formation, use of organofluorosilanes is essential; tetraorganosilanes like aryl(trimethyl)silanes, upon reaction with aryl iodides, gave aroyl fluorides instead. Key Words: carbonylative coupling; organofluorosilanes; ketone synthesis
Palladium-Catalyzed Carbonylactive Coupling of Arylfluorosilanes with Aryl Iodides. A Convenient Synthesis of Diaryl Ketones
Hatanaka, Yasuo,Hiyama, Tamejiro
, p. 2049 - 2052 (2007/10/02)
In the presence of 1 atm of carbon monoxide, arylfluorosilanes activated by potassium fluoride were found to participate in the Pd-catalyzed carbonylactive coupling reaction of aryl iodides to give unsymmetrical diaryl ketones in good yields.
