Repository of Research and Investigative Information

Repository of Research and Investigative Information

Baqiyatallah University of Medical Sciences

Design and Synthesis of Curcumin-Like Diarylpentanoid Analogues as Potential Anticancer Agents

(2016) Design and Synthesis of Curcumin-Like Diarylpentanoid Analogues as Potential Anticancer Agents. Recent Patents on Anti-Cancer Drug Discovery. pp. 342-351. ISSN 1574-8928

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Abstract

Background: Curcumin is a polyphenolic natural compound with multiple targets that used for the prophylaxis and treatment of some type of cancers like cervical and pancreatic cancers. Some recent patent for curcumin for cancer has also been reviewed. Objective: In this study, ten new curcumin derivatives were designed and synthesized and their cytostatic activity evaluated against the Hela and Panc cell lines that some of them showed more activity than curcumin. Method: In the present study, a series of mono-carbonyl derivatives of curcumin were designed and prepared. The details of the synthesis and chemical characterization of the synthesized compounds are described. The cytostatic activities of the designed compounds are assessed in two different tumor cell lines using MTT test. Results: In vitro screening for human cervix carcinoma cell lines (Hela) and pancreatic cell lines (Panc-1) at 24 and 48 hour showed that all the analogs possessed good activity against these tumor cell lines and compounds 5a, 5c and 6 with high potency can be used as a new lead compounds for the designing and finding new and potent cytostatic agents. Docking studies indicated that compound 5c readily binds the active site of human glyoxalase I protein via two strong hydrogen bonds engaging residues of Glu-99 and Lys-156. Conclusion: Our results are useful in guiding a design of optimized ligands with improved pharmacokinetic properties and increased of anti-cancer activity vs. the prototype curcumin compound.

Item Type: Article
Keywords: Cancer curcumin docking MTT 4-piperidone synthesis 14-alpha-demethylase mechanism docking qsar Oncology Pharmacology & Pharmacy
Divisions:
Page Range: pp. 342-351
Journal or Publication Title: Recent Patents on Anti-Cancer Drug Discovery
Journal Index: ISI
Volume: 11
Number: 3
Identification Number: https://doi.org/10.2174/1574892811666160420141613
ISSN: 1574-8928
Depositing User: مهندس مهدی شریفی
URI: http://eprints.bmsu.ac.ir/id/eprint/5183

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