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Molecules 2016, 21(6), 772; doi:10.3390/molecules21060772

Design, Synthesis, and Biological Evaluation of Novel PARP-1 Inhibitors Based on a 1H-Thieno[3,4-d] Imidazole-4-Carboxamide Scaffold

1
Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
2
Department of Neuroimmunopharmacology, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 20 April 2016 / Revised: 4 June 2016 / Accepted: 6 June 2016 / Published: 13 June 2016
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of poly(ADP-ribose)polymerase (PARP)-1 inhibitors containing a novel scaffold, the 1H-thieno[3,4-d]imidazole-4-carboxamide moiety, was designed and synthesized. These efforts provided some compounds with relatively good PARP-1 inhibitory activity, and among them, 16l was the most potent one. Cellular evaluations indicated that the anti-proliferative activities of 16g, 16i, 16j and 16l against BRCA-deficient cell lines were similar to that of olaparib, while the cytotoxicities of 16j and 16l toward human normal cells were lower. In addition, ADMET prediction results indicated that these compounds might possess more favorable toxicity and pharmacokinetic properties. This study provides a basis for our further investigation. View Full-Text
Keywords: PARP-1 inhibitor; BRCA1/2; anti-tumour; thieno[3,4-d]imidazole PARP-1 inhibitor; BRCA1/2; anti-tumour; thieno[3,4-d]imidazole
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Wang, L.; Liu, F.; Jiang, N.; Zhou, W.; Zhou, X.; Zheng, Z. Design, Synthesis, and Biological Evaluation of Novel PARP-1 Inhibitors Based on a 1H-Thieno[3,4-d] Imidazole-4-Carboxamide Scaffold. Molecules 2016, 21, 772.

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