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  • Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.

Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.

Bioorganic & medicinal chemistry (2009-10-06)
Hee-Kyung Rhee, So Yun Lim, Mi-Ja Jung, Youngjoo Kwon, Myung-Hwa Kim, Hea-Young Park Choo
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Doxorubicin hydrochloride, suitable for fluorescence, 98.0-102.0% (HPLC)
Sigma-Aldrich
(S)-(+)-Camptothecin, ≥90% (HPLC), powder
Sigma-Aldrich
Temozolomide, ≥98% (HPLC)
Supelco
Temozolomide, VETRANAL®, analytical standard