Mevithra, M and Chandralekha, S (2020) Molecular docking studies and synthesis of a new class of chroman‑4‑one fused 1,3,4‑thiadiazole derivatives and evaluation for their anticancer potential. Journal of the Iranian Chemical Society.

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Abstract

γ-Secretase inhibitors (GSIs) are repurposed as cancer therapeutics based on the promising inhibition of NOTCH1 signalling
pathway in various cancers. GSIs are a class of small-molecule compounds that target the Notch pathway and have been tested
to treat various types of cancers in preclinical and clinical trials. Although GSIs elicit a response in some tumours as single
agents and sensitize to cytotoxic and targeted therapies, they have not yet been approved for cancer therapy. A new series of
chroman-4-one fused 1,3,4-thiadiazole derivatives has been synthesized with the help of diferent aromatic benzaldehydes,
and the fnal compounds were characterized by FT-IR and 1
HNMR. Chroman-4-one fused 1,3,4-thiadiazole derivatives
were synthesized by the reaction of Schif base derivatives with chroman-4-one fused 1,3,4-thiadiazole. All the synthesized
compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against
MDA-MB-231, MCF-7, and Vero cancer cell lines. Four of the compounds possessed good to moderate anticancer activity.
Four of the synthesized compounds, i.e. 3a, 3c, 3i, and 3e, were found to possess maximum growth inhibition. In conclusion,
the designed chromanone-1,3,4-thiadiazole scafold is an interesting anticancer pharmacophore and considered as novel lead
scafold for any future optimization.

Item Type: Article
Uncontrolled Keywords: Chroman-4-one · 1,3,4-thiadiazole · In vitro anticancer · MDA-MB-231 · MCF-7 and Vero cancer cell lines · Gamma secretase inhibitors
Divisions: PSG College of Arts and Science > Department of Chemistry
Depositing User: Mr Team Mosys
Date Deposited: 16 Aug 2022 04:44
Last Modified: 16 Aug 2022 04:44
URI: http://ir.psgcas.ac.in/id/eprint/1460

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