Design, synthesis, and evaluation of novel 6-chloro-/fluorochromone derivatives as potential topoisomerase inhibitor anticancer agents.
6-Chloro-2-pyrrolidino-/morpholino-/piperidino-/N-methylpiperazino-3-formyl-chromones (13-16) and 6-fluoro-2,7-di-morpholino-/piperidino-/N-methylpiperazino-3-formylchromones (17-19) have been synthesized as potential topoisomerase inhibitor anticancer agents, and evaluated, in vitro, against Ehrlich ascites carcinoma (EAC) cells, and also in vivo on EAC bearing mice. The compounds displayed promising anticancer activity under these test systems and shall serve as useful 'leads' for further design.
Ishar
M P S
MP
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India. mpsishar@yahoo.com
Singh
Gurpinder
G
Singh
Satyajit
S
Sreenivasan
K K
KK
Singh
Gurmit
G
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001835:Body Weight / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D026942:DNA Topoisomerases / Q000378:metabolism; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D051379:Mice; D015394:Molecular Structure; D009368:Neoplasm Transplantation / Q000473:pathology; D013329:Structure-Activity Relationship; D015996:Survival Rate; D059003:Topoisomerase Inhibitors
D000970:Antineoplastic Agents; D002867:Chromones; D004791:Enzyme Inhibitors; D059003:Topoisomerase Inhibitors; D026942:DNA Topoisomerases