Shaikh SA, Wakchaure S, Labhade SR, Kale RR, Alavala RR, Chobe SS, Jain KS, Labhade HS, Bhanushali DD (2024)
Publication Type: Journal article
Publication year: 2024
Book Volume: 18
Article Number: 119
Journal Issue: 1
DOI: 10.1186/s13065-024-01196-1
In an attempt to develop potent anti-cancer agents, a new 1,3,4-substituted-thiadiazole derivatives (8b-g), starting from 4-substituted-thiazol-2-chloroacetamides (4b-g), were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the hepatocellular carcinoma (HEPG-2), human lung carcinoma (A549), human breast carcinoma (MCF-7) and pseudo-normal human embryonic liver (L02) cancer cell lines by an MTT assay. Among all synthesized compounds, compound 8d showed the potent anti-cancer activities with GI50 values of 2.98, 2.85 and 2.53 μM against MCF-7, A549 and HepG-2 cell lines respectively as compared to standard drug Doxorubicin. Furthermore, molecular modelling studies have spotlighted the anchoring role of 1,3,4-substituted-thiadiazole moiety in bonding and hydrophobic interaction with the key amino acid residues. Therefore, these results can provide promising starting points for further development of best anti-cancer agents. Graphical Abstract: (Figure presented.)
APA:
Shaikh, S.A., Wakchaure, S., Labhade, S.R., Kale, R.R., Alavala, R.R., Chobe, S.S.,... Bhanushali, D.D. (2024). Synthesis, biological evaluation, and molecular docking of novel 1,3,4-substituted-thiadiazole derivatives as potential anticancer agent. BMC Chemistry, 18(1). https://doi.org/10.1186/s13065-024-01196-1
MLA:
Shaikh, Samin A., et al. "Synthesis, biological evaluation, and molecular docking of novel 1,3,4-substituted-thiadiazole derivatives as potential anticancer agent." BMC Chemistry 18.1 (2024).
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