147938-34-9

Upstream product

• 110694-61-6 N--L-glutamine ethyl ester 
• 13726-85-7 Boc-Gln-OH 
• 56-85-9 L-glutamine 
• 147938-28-1 N^α--N^δ-<2,2-bis(diethylphosphono)ethyl>glutamine ethyl ester 

Downstream Products

• 147938-31-6 N^α-<4-<(<2,4-diamino-6-pteridinyl>methyl)methylamino>benzoyl>-N^δ-<2,2-bis(diethylphosphono)ethyl>glutamine ethyl ester 
• 147938-30-5 N^α-<4-(methylamino)benzoyl>-N^δ-<2,2-bis(diethylphosphono)ethyl>glutamine ethyl ester 

Relevant academic research and scientific papers

A study of the delivery-targeting concept applied to antineoplastic drugs active on human osteosarcoma. I. Synthesis and biological activity in nude mice carrying human osteosarcoma xenografts of gem-bisphosphonic methotrexate analogues

With the aim of verifying the concept of osteotic vectorisation, synthesis of three methotrexate (MTX) gem-diphosphonic analogues (compounds A, B and C) was performed. These molecules were tested on BALB/c and NIH III mice previously grafted with subcutaneous implants of OHS, TTX p7 and/or TTX p11 human osteosarcoma cell lines. Antineoplasic activity of compound B and C (active compounds) was compared to the activity for MTX alone and to activity of compound A (inactive compound). Compounds B and C exhibited an increased antineoplasic activity compared to MTX alone and to compound A. At equimolar doses, compound B was found to be 5-6-fold more active than MTX given alone. We have discussed the concept of osteotic vectorisation of compound B, which could be regarded as a prodrug.