title: Anticancer activity of novel indenopyridine derivatives.
abstract: Eighteen new 4-[2-amino-3-cyano-5-oxo-4-substitutedaryl-4H-indeno[1,2-b]pyridin-1-(5H)-yl]benzenesulfonamide derivatives 6a-q were synthesized via a reaction of aromatic aldehydes, enaminone 3 and malononitrile in one-pot reaction. Also, compounds 6a-q were obtained, via another route by reaction of enaminone 3 with arylidenemalononitriles 4a-q. The structure of the synthesized compounds was characterized by microanalysis, IR, (1)H-NMR, (13)C-NMR and mass spectral data. All the target compounds were subjected to in vitro anticancer activity against breast cancer cell line (MCF7). Compound 6d showed a higher potency with IC(50) value (4.34 μM) than that of the doxorubicin (5.40 μM), as the reference drug, while compound 6n with IC(50) value (6.84 μM) is nearly as active as doxorubicin. Also, compounds 6a-c, 6e, 6f, 6h and 6p exhibited a moderate activity, while compounds 3, 6g, 6i-m, 6o and 6q showed weak activity.
authors.affiliation: Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. mmsghorab@yahoo.com
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.forename: Mansour S
authors.initials: MS
authors.lastname: Al-Said
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000473:pathology; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000494:pharmacology; D005260:Female; D006801:Humans; D007192:Indenes / Q000138:chemical synthesis / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
chemical_list: D000970:Antineoplastic Agents; D007192:Indenes; D011725:Pyridines; D004317:Doxorubicin