356788-71-1

Upstream product

• 30094-28-1 2-(diethylphosphono)propionic acid 
• 72155-45-4 Boc-L-phenylalaninal 
• 24424-99-5 di-tert-butyl dicarbonate 
• 7524-50-7 methyl (2S)-2-amino-3-phenylpropanoate hydrochloride 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 244033-72-5 (4S)-4-N-tert-butoxycarbonylamino-5-phenyl-2-methyl-2-trans-pentenoic acid, ethyl ester 
• 66605-57-0 (S)-N-tert-butoxycarbonyl-2-amino-3-phenylpropanol 

Downstream Products

• 1219930-75-2 methyl (2S,4R)-2-methyl-4-[({2-[(3R)-4-methyl-3-{methyl[(2S,3S)-3-methyl-2-({[(2R)-1-methylpiperidin-2-yl]carbonyl}amino)pentanoyl]amino}pentyl]-1,3-thiazol-4-yl}carbonyl)amino]-5-phenylpentanoate 
• 1174764-13-6 (2S,4R)-4-[((R)-2-{3-[methyl-(N-methyl-(R)-pipecolyl-(S)-isoleucyl)-amino]-4-methyl-pentyl}-thiazole-4-carbonyl)-amino]-2-methyl-5-phenyl-pentanoic acid trifluoroacetic acid salt 
• 1207472-58-9 methyl (2S,4R)-4-[((R)-2-{3-[(N-benzyloxycarbonyl-(R)-pipecolyl-(S)-isoleucyl)methylamino]-4-methylpentyl}thiazole-4-carbonyl)amino]-2-methyl-5-phenylpentanoate 
• 1207472-62-5 (S,E)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 4-((tert-butoxycarbonyl)amino)-2-methyl-5-phenylpent-2-enoate 
• 796039-50-4 (1R,2'R,1'''R,3'''S)-{1-[2'-{4''-[1'''-benzyl-4'''-(tert-butyldiphenylsilanyloxy)-3'''-methylbutylcarbamoyl]thiazol-2''-yl}-2'-(tert-butyldiphenylsilanyloxy)ethyl]-2-methylpropyl}carbamic acid benzyl ester 
• 796039-49-1 (1R,2'R,1'''R,3'''S)-{1-[2'-{4''-[1'''-benzyl-4'''-(tert-butyldiphenylsilanyloxy)-3'''-methylbutylcarbamoyl]oxazol-2''-yl}-2'-(tert-butyldiphenylsilanyloxy)ethyl]-2-methylpropyl}carbamic acid benzyl ester 
• 796039-52-6 (1R,2'R,1''R,3''S)-acetic acid 1-{4'-[1''-benzyl-4''-(tert-butyldiphenylsilanyloxy)-3''-methylbutylcarbamoyl]thiazol-2'-yl}-3-benzyloxycarbonylamino-4-methylpentyl ester 
• 796039-51-5 (1R,2'R,1'''R,3'''S)-[1-(2'-{4''-[1'''-benzyl-4'''-(tert-butyldiphenylsilanyloxy)-3'''-methylbutylcarbamoyl]thiazol-2''-yl}-2'-hydroxyethyl)-2-methylpropyl]carbamic acid benzyl ester 
• 796039-55-9 (1R,3R,1''R,3''S)-acetic acid 1-[4'-(1''-benzyl-4''-hydroxy-3''-methylbutylcarbamoyl)thiazol-2'-yl]-3-benzyloxycarbonylamino-4-methylpentyl ester 

Relevant academic research and scientific papers

Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Synthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic

Total Synthesis and Biological Evaluation of Tubulysin Analogues

We report a second-generation synthesis of the exceedingly potent antimitotic agent N14-desacetoxytubulysin H (1) as well as the preparation of nine analogues of this lead structure. Highlights of our synthetic efforts include an efficient late

BIOACTIVE PRE-TUBULYSINS AND USE THEREOF

The invention relates to bioactive pre-tubulysin derivatives, their preparation and pharmacological use.

Synthesis and biological evaluation of pretubulysin and derivatives

Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in the subnanomolar range towards various tumor cell lines. Its activity is only slightly less than those of the structurally more complex tubulysins. With a straig

Synthesis of the tubuvaline-tubuphenylalanine (Tuv-Tup) fragment of tubulysin

(Chemical Equation Presented) Advanced intermediates and analogues of tubulysins were prepared in a convergent strategy.

Stereoselective synthesis of vinylogous peptides

A trans or cis ethenyl group has been inserted between the α-carbon and the carboxyl group of α-aminoacids by Horner stereoselective olefination of α-aminoaldehydes. Numerous pure cis and trans vinylogous α-aminoacids have been obtained thus and coupled w