The present invention relates to compds. I [n and m = (independently) 0-8; Q = (un)substituted aryl, nitrogen-contg. heterocyclel; W = NR, divalent monoglycosyl, piperidinediyl, piperazinediyl or pyrrolidinediyl; X1 = O or NR1; X2 = O, NR2 or a bond; X3 = N, NR3; X4 = O, NR4, OR4, NR4R5; Y1 and Y2 = (independently) halo, H, (un)substituted aryl, etc. (provided that at least one of Y1 and Y2 represent a group other than H); R = H, CHO, CO2(alkyl), etc.; R1 and R2 = (independently) H, alkyl; R3 and R4 = (independently) H, alkyl, aryl, etc.; R5 = H, alkyl] and pharmaceutically acceptable salts and solvates thereof, their methods of prepn., their use as a drug, notably in the treatment of cancer, and pharmaceutical compns. contg. such compds. Eight compds. I were prepd. E.g., a multi-step synthesis of II, starting from 4-chloroquinoline and ethanolamine, was described. Exemplified compds. I were tested for DNMT1 inhibition and DNMT3A inhibition (data given). [on SciFinder(R)]
Halby, L., Arimondo, P., Mai, A., Rotili, D. (2015)Preparation of substituted quinazoline derivatives as DNA methyltransferase inhibitors. . Brevetto No. WO 2016/151144 Al.
Preparation of substituted quinazoline derivatives as DNA methyltransferase inhibitors
Rotili, Dante.
2015-01-01
Abstract
The present invention relates to compds. I [n and m = (independently) 0-8; Q = (un)substituted aryl, nitrogen-contg. heterocyclel; W = NR, divalent monoglycosyl, piperidinediyl, piperazinediyl or pyrrolidinediyl; X1 = O or NR1; X2 = O, NR2 or a bond; X3 = N, NR3; X4 = O, NR4, OR4, NR4R5; Y1 and Y2 = (independently) halo, H, (un)substituted aryl, etc. (provided that at least one of Y1 and Y2 represent a group other than H); R = H, CHO, CO2(alkyl), etc.; R1 and R2 = (independently) H, alkyl; R3 and R4 = (independently) H, alkyl, aryl, etc.; R5 = H, alkyl] and pharmaceutically acceptable salts and solvates thereof, their methods of prepn., their use as a drug, notably in the treatment of cancer, and pharmaceutical compns. contg. such compds. Eight compds. I were prepd. E.g., a multi-step synthesis of II, starting from 4-chloroquinoline and ethanolamine, was described. Exemplified compds. I were tested for DNMT1 inhibition and DNMT3A inhibition (data given). [on SciFinder(R)]I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.