Synlett
DOI: 10.1055/a-2531-7183
letter
Small Molecules in Medicinal Chemistry

Synthesis and Evaluation of Bakuchiol-Tethered Triazoles as Cytotoxic Agents

Neha Sengar
a   Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab, 160062, India
,
Joydeep Chatterjee
b   Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, 151401, India
,
Raj Kumar∗
b   Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, 151401, India
,
Inder Pal Singh∗
a   Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab, 160062, India
› Author AffiliationsNS is thankful to the National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, the Ministry of Chemicals and Fertilizers, India for the award of junior and senior research fellowships. RK and JC thank Council of Scientific and Industrial Research, India (CSIR, 02/0397/2021/EMR-II) for financial support.
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Abstract

A novel series of bakuchiol-tethered triazole compounds was synthesized by reaction of azido bakuchiol with different substituted alkynes. The anticancer activity of all synthesized compounds was evaluated against A549 (lung), MCF-7, and MDA-MB-231 (breast) human tumor cells. Cytotoxicity screening showed that several compounds displayed notable cytotoxic effects against tumor cells compared to the parent molecule bakuchiol. The prominent effects were produced by compounds with IC50 values of 8.9 μM and 8.2 μM against the MCF-7 and A-549 cells, respectively.

Key words

anticancer - bakuchiol - triazole - click chemistry - semisynthetic - cancer

Supporting Information

    Supporting information for this article is available online at https://doi.org/10.1055/a-2531-7183.
  • Supporting Information


Publication History

Received: 02 December 2024

Accepted after revision: 03 February 2025

Accepted Manuscript online:
03 February 2025

Article published online:
21 March 2025

© 2025. Thieme. All rights reserved

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