Evaluation of apoptosis-induction by newly synthesized phthalazine derivatives in breast cancer cell lines.
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.
Arif
Jamal M
JM
Biological and Medical Research, King Faisal Specialist Hospital and Research Center, Riyadh 11211, Saudi Arabia. arifjm@yahoo.com
Kunhi
Muhammad
M
Bekhit
Adnan A
AA
Subramanian
Manogaran P
MP
Al-Hussein
Khalid
K
Aboul-Enein
Hassan Y
HY
Al-Khodairy
Fahad M
FM
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*
D008024:Ligands; D010793:Phthalazines; D017671:Platinum Compounds; D003300:Copper; C043388:phthalazine