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

Rhee, Hee-Kyung; Lim, So Yun; Jung, Mi-Ja; Kwon, Youngjoo; Kim, Myung-Hwa; Choo, Hea-Young Park

doi:10.1016/j.bmc.2009.09.014

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

Rhee, Hee-Kyung;
Lim, So Yun;
Jung, Mi-Ja;
Kwon, Youngjoo;
Kim, Myung-Hwa;
외 1명

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22

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25

초록

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. (C) 2009 Elsevier Ltd. All rights reserved.

키워드

PARP-1; Isoquinolinone; Cytotoxic potentiation; POLY(ADP-RIBOSE) POLYMERASE; DISCOVERY; ABT-888; AGENTS

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

저자: Rhee, Hee-Kyung; Lim, So Yun; Jung, Mi-Ja; Kwon, Youngjoo; Kim, Myung-Hwa; Choo, Hea-Young Park

DOI: 10.1016/j.bmc.2009.09.014

발행일: 2009-11-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry

권: 17

호: 21

페이지: 7537 ~ 7541

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 5 페이지

ISSN: E 1464-3391
P 0968-0896