174487-86-6

Upstream product

• 197223-64-6 dimethyl N-[N-(benzyloxycarbonyl)-L-γ-glutamyl]-glycinate 
• 30134-53-3 S-4-Cyano-2-[[(phenylmethoxy)carbonyl]-amino]butanoic acid methyl ester 
• 96-32-2 bromoacetic acid methyl ester 
• 65882-90-8 methyl (2S)-2-(benzyloxycarbonylamino)-4-(tetrazol-5-yl)butyrate 

Downstream Products

• 197223-58-8 methyl (2S)-2-[4-[N-[(3,4-dihydro-2,7-dimethyl-4-oxo-6-quinazolinyl)methyl]-N-prop-2-ynylamino]-2-fluorobenzamido]-4-(1-methoxycarbonylmethyltetrazol-5-yl)butyrate 

Relevant academic research and scientific papers

Anti-cancer compounds

Cyclopentaquinazoline of the formula (I): STR1 wherein R1 is hydrogen, amino, C1-4 alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl or C1-4 fluoroalkyl; wherein R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and wherein R3 is a group of the formula: in which A1, A2, Y1 and Ar2 are defined in claim 1; or a pharmaceutically acceptable salt or ester there of are of therapeutic value particularly in the treatment of cancer.

Synthesis of novel quinazoline-based antifolates with modified glutamate side chains as potential inhibitors of thymidylate synthase and antitumour agents

Several novel antifolates, derivatives of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid, were synthesised as inhibitors of thymidylate synthase (TS) and antitumour agents. This was accomplished by first developing routes to the key in