Xi, Wenli published the artcileIdentification of Novel 4′-O-Demethyl-epipodophyllotoxin Derivatives as Antitumor Agents Targeting Topoisomerase II, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is demethylepipodophyllotoxin preparation antitumor topoisomerase II inhibitor; 4′-O-demethyl-epipodophyllotoxin; antitumor agent; topoisomerase II.
C4 variation of 4′-O-demethyl-epipodophyllotoxin (DMEP) I is an effective approach to optimize the antitumor spectra of this compound class. Accordingly, two series of novel DMEP derivatives were synthesized, and as expected, the antitumor spectra of these derivatives varied with different C4 substituents. Notably, most compounds showed significant inhibition against the etoposide (2)-resistant KBvin cells. Four of the compounds I (R = [4-[3-(dimethylamino)propanamido]phenyl]aminyl, (4-[3-[benzyl(methyl)amino]propanamido]phenyl)aminyl, [1-[(4-fluorophenyl)methyl]piperidin-4-yl]amidyl and 3-[benzyl(methyl)amino]propanamidyl) induced protein-linked DNA break (PLDB) levels higher than those of GL-331 I (R = (4-nitrophenyl)aminyl), and are assumed to be topoisomerase II (topo II) poisons more potent than I (R = (4-nitrophenyl)aminyl) and 2. Compound I (R = 3-[benzyl(methyl)amino]propanamidyl), a potent topo II poison highly effective against KBvin cells, was further evaluated with a panel of tumor cells and was most active against HepG2. This compound also exhibited apparent in vivo antitumor efficacy in hepatoma 22 (H22) mouse model. The results indicated that C4 derivation of DMEP is a feasible approach to identify potent topo II inhibitors with optimized antitumor profiles.
Molecules published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem