Key points are not available for this paper at this time.
Abstract 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 GI 50 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
Shaikh et al. (Thu,) studied this question.