Fu, Zhangyu published the artcileDesign, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure, Recommanded Product: N-Methoxy-N-methylisonicotinamide, the publication is Bioorganic & Medicinal Chemistry (2018), 26(8), 2061-2072, database is CAplus and MEDLINE.
Based on the co-crystal structures of tubulin with plinabulin and Compound 1 ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-benzoylbenzylidene)piperazine-2,5-dione, a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biol. activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-(thiophene-3-carbonyl)benzylidene)piperazine-2,5-dione) and 13e ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-(thiophene-2-carbonyl)benzylidene)piperazine-2,5-dione) exhibited potent activities with IC50 at 1.56 and 1.72 nM, resp. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization Furthermore, the interaction between tubulin and these compounds were elucidated by mol. 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 Phe 20, which could enhance their binding affinities.
Bioorganic & Medicinal Chemistry published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Recommanded Product: N-Methoxy-N-methylisonicotinamide.
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