Nicolaou, K. C. published the artcileSynthesis and Biological Evaluation of Shishijimicin A-Type Linker-Drugs and Antibody-Drug Conjugates, Name: 2-Methyl-2-sulfanylpropan-1-ol, the publication is Journal of the American Chemical Society (2020), 142(29), 12890-12899, database is CAplus and MEDLINE.
Our previous studies with shishijimicin A resulted in the total synthesis of this scarce marine natural product and a number of its simpler analogs endowed with picomolar potencies against certain cancer cell lines. Herein, we describe the design, synthesis, and biol. evaluation of four linker-drugs, anticipating the construction of antibody-drug conjugates (ADCs) as the ultimate goal of this research program. Using a common payload, the assembly of these linker-drugs utilized different linkers and attachment points, providing opportunities to probe the optimal mol. design of the intended ADCs as targeted cancer therapies. In the course of ADC generation and in vitro evaluation, we identified two linker-drugs with a promising in vitro plasma stability profile and excellent targeted cytotoxicity and specificity. Conjugation of shishijimicin A enediyne payloads through their phenolic moiety represents a novel approach to enediyne ADC creation, while the pharmacol. profiles of at least two of the generated ADCs compare well with the profiles of the corresponding clin. approved ADC Kadcyla.
Journal of the American Chemical Society published new progress about 73303-88-5. 73303-88-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Alcohol, name is 2-Methyl-2-sulfanylpropan-1-ol, and the molecular formula is C4H10OS, Name: 2-Methyl-2-sulfanylpropan-1-ol.
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