148565-06-4

Upstream product

• 120205-51-8 tert-butyl N-[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]carbamate 
• 133645-51-9 (4R,5S,2'R,3'R,2S)-3-[3'-(N-tert-butoxycarbonyl-2-pyrrolidinyl)-3-hydroxy-2'-methylpropanoyl]-4-methyl-5-phenyl-2-oxazolidinone 
• 133565-36-3 (S)-benzyl 2-phenyl-1-(thiazol-2-yl)ethylcarbamate 
• 163768-51-2 benzyl (2R,3R,2'S)-3-(N-tert-butoxycarbonyl-2'-pyrrolidinyl)-3-hydroxy-2-methylpropanoate 
• 69610-41-9 Boc-L-Pro-H 

Downstream Products

• 148683-12-9 Boc-(3R,4S,5S)-bisnorDil-(2R,3R,4S)-norDap-(S)-Doe 

Relevant academic research and scientific papers

Stereoselective Synthesis of Dolastatin 10 and Its Congeners

Efficient synthesis of dolastatin 10 (1), a potent antitumor peptide from a sea hare Dolabella auricularia, has been achieved in a stereoselective manner.Trisnordolastatin 10 (2) and its C9-epimer (3) have also been synthesized.

Synthesis and antitumor activity of novel dolastatin 10 analogs

Dolastatin 10 (1) is a potent antineoplastic pentapeptide. Novel dolastatin 10 analogs each modified at one of the constituent amino acid derivatives, were synthesized and their antitumor activity was evaluated against P388 leukemia in mice. The structural requirements for antitumor activity are discussed. Some of the analogs, 31c, 35c, 38b, and 50c showed excellent activity in vivo. Highly active 50c, which lacks the thiazole group of 1, was selected for further development as an antitumor agent.