Synthesis and evaluation of pyrazole‐incorporated monocarbonyl curcumin analogues as antiproliferative and antioxidant agents

A series of pyrazole‐incorporated monocarbonyl analogues of curcumin were synthesized via Clasien–Schimidt‐type condensation and subsequently screened for in vitro antiproliferative and antioxidant activity. The analogues 4c, 5d, 5e, 5g, 6e, and 6f showed potential activity against the MDA‐MB‐231 ce...

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Published inJournal of the Chinese Chemical Society (Taipei) Vol. 66; no. 12; pp. 1658 - 1665
Main Authors Nagargoje, Amol A., Akolkar, Satish V., Siddiqui, Madiha M., Bagade, Aditi V., Kodam, Kisan M., Sangshetti, Jaiprakash N., Damale, Manoj G., Shingate, Bapurao B.
Format Journal Article
LanguageEnglish
Published Weinheim Wiley‐VCH Verlag GmbH & Co. KGaA 01.12.2019
Wiley Subscription Services, Inc
Subjects
antioxidant activity
Antioxidants
Antiproliferative activity
Antiproliferatives
Ascorbic acid
Molecular docking
Monocarbonyl curcumin analogues
Pyrazole
Scavenging
Synthesis
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Summary:A series of pyrazole‐incorporated monocarbonyl analogues of curcumin were synthesized via Clasien–Schimidt‐type condensation and subsequently screened for in vitro antiproliferative and antioxidant activity. The analogues 4c, 5d, 5e, 5g, 6e, and 6f showed potential activity against the MDA‐MB‐231 cell line. The synthesized analogues were also screened for their antioxidant activity. Compounds 5a, 5e, 6d, and 6f exhibit comparable radical scavenging activity with respect to the standard drug ascorbic acid. Furthermore, a molecular docking study has been conducted for 5d and 5g and suggests that these compounds have a potential to become lead molecules in drug discovery and process. Pyrazole incorporated monocarbonyl analogues of curcumin were synthesized and evaluated for their in vitro antiproliferative and antioxidant activity.
ISSN:0009-4536
2192-6549
DOI:10.1002/jccs.201800405