Synthesis, cytotoxicity and SAR of simple geiparvarin analogues.
Some simple geiparvarin analogues, in which the coumarin moiety has been replaced with an X-substituted benzene ring, are described. The compounds were tested on LoVo cells (human colon carcinoma cell line) and some of them show a cytotoxicity comparable with that of the prototype. A QSAR analysis was also attempted, but it did not provide satisfactory results, mainly because of the limited range of variation of the biological activity.
Valenti
P
P
Department of Pharmaceutical Sciences, University of Bologna, Italy.
Rampa
A
A
Recanatini
M
M
Bisi
A
A
Belluti
F
F
Da Re
P
P
Carrara
M
M
Cima
L
L
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003110:Colonic Neoplasms / Q000473:pathology; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D003374:Coumarins; C058446:geiparvarin