Journal
BIOORGANIC CHEMISTRY
Volume 91, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.103181
Keywords
PARP-1; Antitumor; Chemosensitizer; Inhibitor
Funding
- National Natural Science Foundation of China [21672260, 21372260]
- Natural Science Foundation of Jiangsu Province of China [BK20170743]
- Fundamental Research Funds for the Central Universities, China [2632017PY13]
- College Students Innovation Project for the RAMP
- D of Novel Drugs [J1310032]
- National Found for Fostering Talents of Basic Science (NFFTBS)
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Two new series of compounds were designed and synthesized as potent PARP-1 inhibitors. These compounds were evaluated for PARP-1 enzyme and cellular inhibitory activities. All efforts lead to the identification of 9k (named as LG-12) with efficient potency both for PARP-1 and BRCA1 deficient MDA-MB-436 cells. Additionally, the novel PARP-1 inhibitor LG-12 is an efficient chemosensitizer, which could potentiate the anti-cancer effect of TMZ. Our data presented herein provide a comprehensive preclinical in vitro evaluation of the potential therapeutic efficacy and potency of chemotherapeutic agent-PARP-1 inhibitor combinations for LG-12. The combined results indicated that LG-12 could be a promising candidate for further study.
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