Synthesis of antineoplaston A10 analogs as potential antitumor agents.
Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.
Choi
B G
BG
College of Pharmacy, Chonnam National University, Kwangju, Korea.
Kim
O Y
OY
Chung
B H
BH
Cho
W J
WJ
Cheon
S H
SH
Choi
S U
SU
Lee
C O
CO
D000970:Antineoplastic Agents / Q000494:pharmacology*; D044482:Benzeneacetamides; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006865:Hydrogenation; D010881:Piperidones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D044482:Benzeneacetamides; D010881:Piperidones; C052091:antineoplaston A10