218288-94-9

Upstream product

• 131148-64-6 (S)-ethyl 2-(1-(tert-butoxycarbonylamino)-2-phenylethyl)thiazole-4-carboxylate 
• 72155-45-4 Boc-L-phenylalaninal 
• 1026007-03-3 C₁₉H₂₆N₂O₅S 
• 99281-95-5 tert-butyl [(2S)-1-amino-3-phenyl-1-thioxopropan-2-yl]carbamate 
• 88463-18-7 (S)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropionamide 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 218288-92-7 (R)-2-((S)-1-tert-Butoxycarbonylamino-2-phenyl-ethyl)-thiazolidine-4-carboxylic acid ethyl ester 
• 87694-53-9 Boc-Phe-OH N,O-dimethyl hydroxamate 
• 3411-58-3 L-cystein ethyl ester 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 

Downstream Products

• 1414375-90-8 EtO-Thiazole-Phe-Val-NHBoc 
• 1414375-74-8 San B 7 

Relevant academic research and scientific papers

Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations

Dolastatin 10 (1) is a highly potent cytotoxic microtubule inhibitor (cytotoxicity IC50 5.0 nM) and several of its analogs have recently been used as payloads in antibody drug conjugates. Herein, we describe the design and synthesis of a series of novel dolastatin 10 analogs useful as payloads for conjugated drugs. We explored analogs containing functional groups at the thiazole moiety at the C-terminal of dolastatin 10. The functional groups included amines, alcohols, and thiols, which are representative structures used in known conjugated drugs. These novel analogs showed excellent potency in a tumor cell proliferation assay, and thus this series of dolastatin 10 analogs is suitable as versatile payloads in conjugated drugs. Insights into the structure–activity relationships of the analogs are also discussed.

Synthesis, structurea-activity analysis, and biological evaluation of sanguinamide B analogues

We report the first synthesis of sanguinamide B analogues. Substituting N-methylated (N-Me) amino acids, glycine (Gly), and l-or d-phenylalanine (Phe) into the backbone of sanguinamide B showed that only l-and d-Phe residues controlled the macrocycle conf

Synthesis and antiproliferative activity of a cyclic analog of dolastatin 10

A cyclic analog of the natural antiproliferative compound dolastatin 10 was synthesized by introducing an ester link between the N- and C-terminal residues which were modified accordingly. The final macrolactonization was performed by using isopropenyl chloroformate and DMAP as reagents. This analog exhibits submicromolar antiproliferative activity against the L1210 and HT29 cell lines and inhibits in vitro tubulin polymerization (IC50, 39 μM).