The preparation and in vitro antiproliferative activity of phthalimide based ketones on MDAMB-231 and SKHep-1 human carcinoma cell lines.
The 'one pot' condensation reaction for the synthesis and potent antiproliferative inhibition of alpha-phthalimide based ketones is reported here. 2-Phthalimide-1-(4-fluoro-phenyl)ethanone (5) showed the best growth inhibition on human MDAMB-231 breast carcinoma and SKHep-1 hepatoma cell lines. Preliminary studies showed that the reported bioactivity may be due to the presence of strong electronegative fluorine group at the para-position of the aryl ring.
Chan
Sau Hing
SH
Lo Ka Chung Centre for Natural Anti-cancer Drug Development (Laboratory B), Departement of Applied Biology and Chemical Technology, Institute of Textiles and Clothing, Hong Kong Polytechnic University, 852 Hong Kong, China.
Lam
Kim Hung
KH
Chui
Chung Hin
CH
Gambari
Roberto
R
Yuen
Marcus Chun Wah
MC
Wong
Raymond Siu Ming
RS
Cheng
Gregory Yin Ming
GY
Lau
Fung Yi
FY
Au
Yiu Kwok
YK
Cheng
Chor Hing
CH
Lai
Paul Bo Shan
PB
Kan
Chi Wai
CW
Kok
Stanton Hon Lung
SH
Tang
Johnny Cheuk On
JC
Chan
Albert Sun Chi
AS
D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009369:Neoplasms / Q000473:pathology*; D010797:Phthalimides / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D007659:Ketones; D010797:Phthalimides