160060-21-9Relevant articles and documents
TUBULYSINS AND PROTEIN-TUBULYSIN CONJUGATES
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Paragraph 0014; 00307, (2020/07/14)
Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with cancer, including tubulysins and protein (e.g., antibody) drug conjugates thereof.
Synthesis method of 2-acetyl thiazole-4-ethyl formate
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Paragraph 0023; 0025-0030; 0041-0044; 0049-0056, (2017/11/04)
The invention discloses a synthesis method of 2-acetyl thiazole-4-ethyl formate. The method comprises the following steps: (1) adding L-cysteine ethyl ester hydrochloride, a methylglyoxal water solution, inorganic base and a phase transfer catalyst into a solvent system under nitrogen protection for carrying out a cyclization reaction; (2) separating an organic phase out of reaction products obtained in the step (1) under nitrogen protection, and mixing the organic phase with manganese dioxide for carrying out an oxidizing reaction; (3) purifying the product obtained in the step (2) to obtain the 2-acetyl thiazole-4-ethyl formate. The synthesis method provided by the invention is simple to operate, high in yield and low in cost.
Synthesis and cytotoxicity evaluation of diastereoisomers and N-terminal analogues of tubulysin-U
Shankar, P. Sreejith,Bigotti, Serena,Lazzari, Paolo,Manca, Ilaria,Spiga, Marco,Sani, Monica,Zanda, Matteo
, p. 6137 - 6141 (2013/10/22)
Tubulysins are potent anti-mitotic natural compounds and a scalable and efficient synthetic route for generation of its analogues has been developed and extended to the synthesis of diastereoisomers and N-terminal analogues of tubulysin-U. Structure-activ