Abstract
Rucaparib and PJ34 were used as the structural model for the design of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units. And target compounds were successfully synthesized through a 3-step synthetic strategy. All target compounds were screened for their anti-proliferative effects against OVCAR-3 cell line. Preliminary biological study of these compounds provided potent compounds d21 and d22 with better activities than Rucaparib.
Keywords:
5H-dibenzo[b,e]azepine-6,11-dione; Anticancer; PARP-1 inhibitors.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Azepines / chemical synthesis
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Azepines / chemistry
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Azepines / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Design*
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Drug Screening Assays, Antitumor
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Humans
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Molecular Structure
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Oxadiazoles / chemistry
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Oxadiazoles / pharmacology*
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Structure-Activity Relationship
Substances
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5H-dibenzo(b,e)azepine-6,11-dione
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Antineoplastic Agents
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Azepines
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Oxadiazoles
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1,3,4-oxadiazole