627093-70-3

Upstream product

• 399017-30-2 4-dimethylaminomethylene-6-methyl-4H-pyrano[4,3-b]quinoline-1,3-dione 
• 214360-73-3 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)aniline 

Downstream Products

• 214360-73-3 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)aniline 
• 627093-85-0 N-[2-(dimethylamino)ethyl]-6-methyl-1-oxo-2-[4-(4,4,5,5-tetramethyl[1,3,2]dioxaborolan-2-yl)phenyl]-1,2-dihydrobenzo[b][1,6]naphthyridine-4-carboxamide 

Relevant academic research and scientific papers

Synthesis and cytotoxic activity of carboxamide derivatives of benzo[b][1,6]naphthyridin-(5H)ones

A previous reaction leading to 2-substituted 6-methyl-1-oxo-1,2- dihydrobenzo[b][1,6]naphthyridine-4-carboxylic acids has been extended to encompass a broad range of 2-substituents. Derived carboxamides, particularly 4-N-[2-(dimethylamino)ethyl], were tested for growth inhibitory properties. Potent cytotoxicity against murine P388 leukemia and Lewis lung carcinoma (LLTC) was retained for compounds bearing a remarkably diverse range of 2-substituents with a number having IC50 values 10 nM. Five of the new compounds were tested in vivo against subcutaneous colon 38 tumors in mice; a single dose (1.8 mg/kg) proved curative for the 2-(4-fluorophenyl) derivative, a further increase in potency over the very effective 2-methyl analogue reported previously.

ANTI-TUMOUR POLYCYCLIC CARBOXAMIDES

This invention relates to polycyclic carboxamide compounds of the formula (I) with cytotoxicity, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and/or prophylaxis of cellular proliferative disorders such as cancer.