Nicolaou, K. C. published the artcileImproved Total Synthesis of Tubulysins and Design, Synthesis, and Biological Evaluation of New Tubulysins with Highly Potent Cytotoxicities against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates, Category: esters-buliding-blocks, the publication is Journal of the American Chemical Society (2018), 140(10), 3690-3711, database is CAplus and MEDLINE.
Improved, streamlined total syntheses of natural tubulysins such as V and U, I (R = β-OH, β-OAc, resp.), and pretubulysin D I (R = H), and their application to the synthesis of designed tubulysin analogs, are described. Cytotoxicity evaluation of the synthesized compounds against certain cancer cell lines revealed a number of novel analogs with exceptional potencies [e.g., II: IC50 = 40 pM against MES SA (uterine sarcoma) cell line; IC50 = 6 pM against HEK 293T (human embryonic kidney cancer) cell line; and IC50 = 1.54 nM against MES SA DX (MES SA with marked multidrug resistance) cell line]. These studies led to a set of valuable structure-activity relationships that provide guidance to further mol. design, synthesis, and biol. evaluation studies. The extremely potent cytotoxic compounds discovered in these investigations are highly desirable as potential payloads for antibody-drug conjugates and other drug delivery systems for personalized targeted cancer chemotherapies.
Journal of the American Chemical Society published new progress about 251320-63-5. 251320-63-5 belongs to esters-buliding-blocks, auxiliary class Aliphatic Chain, name is (S)-tert-Butyl (1-hydroxy-3-methylbutan-2-yl)(methyl)carbamate, and the molecular formula is C11H23NO3, Category: esters-buliding-blocks.
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https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics