title: Evaluation of apoptosis-induction by newly synthesized phthalazine derivatives in breast cancer cell lines.
abstract: Newly synthesized phthalazine derivatives including copper and platinum complexes were evaluated for cytotoxicity in human breast cancer cell lines. The cells were incubated with the compounds (100 microM) for 72 h and cytotoxicity, apoptosis and DNA content were measured by flow cytometery. Our results suggest that the parent (H1-2), copper (C1-2)- and platinum (P1-2)-derivatized compounds were relatively more active in inducing apoptosis and cell killing in both human breast cancer cell lines, MDA-MB-231 cells being the more sensitive. Other compounds showed weak or no response towards these parameters except H-5 causing 40% apoptosis in MDA-MB-231 cells. Addition of copper or platinum in the structures generally reduced the apoptotic potential. Possible roles for structure activity relationships are discussed.
authors.affiliation: Biological and Medical Research, King Faisal Specialist Hospital and Research Center, Riyadh 11211, Saudi Arabia. arifjm@yahoo.com
authors.forename: Jamal M
authors.initials: JM
authors.lastname: Arif
authors.forename: Muhammad
authors.initials: M
authors.lastname: Kunhi
authors.forename: Adnan A
authors.initials: AA
authors.lastname: Bekhit
authors.forename: Manogaran P
authors.initials: MP
authors.lastname: Subramanian
authors.forename: Khalid
authors.initials: K
authors.lastname: Al-Hussein
authors.forename: Hassan Y
authors.initials: HY
authors.lastname: Aboul-Enein
authors.forename: Fahad M
authors.initials: FM
authors.lastname: Al-Khodairy
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000473:pathology*; D002277:Carcinoma / Q000473:pathology*; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003300:Copper / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008024:Ligands; D010793:Phthalazines / Q000737:chemistry / Q000494:pharmacology*; D017671:Platinum Compounds / Q000494:pharmacology*
chemical_list: D008024:Ligands; D010793:Phthalazines; D017671:Platinum Compounds; D003300:Copper; C043388:phthalazine