Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.
The isoquinolinone-based tetracyclic compounds were designed and synthesized and their PARP-1 inhibitory activity was evaluated. Most of synthesized compounds showed fairly good activity. Also the most active compound 6 showed its activity on potentiation of anticancer agents, temozolamide and etoposide, by 1.7 times, respectively.
Department of Biological Science, Sookmyung Women's University, Seoul, Republic of Korea.
Hee-Kyung
HK
Rhee
So Yun
SY
Lim
Mi-Ja
MJ
Jung
Youngjoo
Y
Kwon
Myung-Hwa
MH
Kim
Hea-Young Park
HY
Choo
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D004249:DNA Damage; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D015363:Quinolones / Q000737:chemistry*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D006576:Heterocyclic Compounds, 4 or More Rings; D007546:Isoquinolines; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D015363:Quinolones; C545775:methyl-6H-pyrido(2',1'-1,2)imidazo(5,4-c)isoquinolin-5-one; D011065:Poly(ADP-ribose) Polymerases