Synthesis and biological evaluation of 1,2,3-triazole hybrids of 4-methoxy ethyl cinnamate isolated from Hedychium spicatum (Sm) rhizomes: identification of antiproliferative lead actives against prostate cancer

A series of 1, 2, 3- triazole hybrids (9a-9n) were synthesised from major phenolic constituent, 4-methoxy ethyl cinnamate (5) isolated from rhizomes of Hedychium spicatum (Sm), a traditional medicinal plant used in variety of disease conditions. All the synthesised analogues were tested for their in...

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Bibliographic Details
Published in:Natural product research 2023, Vol.37 (2), p.289-295
Main Authors: Kumari, G. Swarna, Siva, Bandi, Reddy, S. Divya, Nayak, V. Lakshma, Tiwari, Ashok K., Rao, Bhattu Ganga, Babu, K. Suresh
Format: Article
Language:English
Subjects:
1,2,3-triazole
Antineoplastic Agents - pharmacology
antiproliferative
Antiproliferatives
Apoptosis
Aquatic plants
Cell cycle
Cell Line, Tumor
Cell Proliferation
Colon cancer
Doxorubicin
Drug Screening Assays, Antitumor
Flow cytometry
Hedychium
Hedychium spicatum
HEK293 Cells
Hepatoma
Herbal medicine
Humans
Hybrids
hydroxycinnamic acids
Lung cancer
Male
Medicinal plants
Phenolic compounds
Phenols
Prostate cancer
Prostatic Neoplasms - drug therapy
Rhizome
Rhizomes
Structure-Activity Relationship
Triazoles
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Summary:A series of 1, 2, 3- triazole hybrids (9a-9n) were synthesised from major phenolic constituent, 4-methoxy ethyl cinnamate (5) isolated from rhizomes of Hedychium spicatum (Sm), a traditional medicinal plant used in variety of disease conditions. All the synthesised analogues were tested for their in vitro antiproliferative potential against HCT 116 (colon cancer), A549 (lung cancer), DU-145 (prostate cancer), Hep G2 (hepatoma) and HEK-293 (normal) cell lines. Among the compounds tested, compounds 9i and 9k potently arrested proliferation of DU-145 (prostate cancer) cell line. Compound 9i displayed 20 times better antiproliferative potential than parent compound and almost identical inhibitory activity to that of the standard drug, doxorubicin. The flow cytometric analysis revealed that 9i arrested cells in G2/M phase of cell cycle and induced apoptosis. Overall, the hybrid derivative 9i was found to be a potential antiproliferative lead against prostate cancer.
ISSN:1478-6419
1478-6427
DOI:10.1080/14786419.2021.1969928