Cytotoxic potential of novel 6,7-dimethoxyquinazolines.
Herein, we report the synthesis and cytotoxicity of a series of substituted 6,7-dimethoxyquinazoline derivatives. The cytotoxic activity of all synthesized compounds has been evaluated against HCT116p53(+/+) and HCT116p53(-/-) colon cancer cells and a HEY ovarian cancer cell line naturally resistant to cisplatin. Nine of the tested compounds showed significant cytotoxicity in all cell lines at 10μM. The most promising derivative (7c) showed IC(50)values of 0.7 and 1.7μM in the two colon cancer cell lines.
Pharmacy Department, The M.S. University of Baroda, Vadodara, 390001 Gujarat, India. mryadav11@yahoo.co.in
Mange R
MR
Yadav
Fedora
F
Grande
Bishram S
BS
Chouhan
Prashant P
PP
Naik
Rajani
R
Giridhar
Antonio
A
Garofalo
Nouri
N
Neamati
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy*; D005260:Female; D045325:HCT116 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010051:Ovarian Neoplasms / Q000188:drug therapy*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011799:Quinazolines