Synthesis of new calix[4]arene derivatives and evaluation of their cytotoxic activity

Since calixarenes are more easily synthesized and functionalized than other supramolecules, they compounds of interest in organic chemistry. In this study, the dihydrazide (3a 3b) diamino propyl (6a 6b) derivatives p-tert-butylcalix[4]arene calix[4]arene were synthesized. Then L-proline methyl ester substituted chlorocyclopropenium was reacted with (3a, 3b, 6a, at room temperature CH2Cl2 to obtain superbase (4a, 4b, 7a, 7b) 75%, 60%, 70%, 55% yield, respectively. The compounds’ structure elucidated using spectroscopic techniques (FTIR, 1H NMR, 13C NMR). cytotoxic properties investigated against different human cancer cell, including A549, DLD-1, HEPG2, PC-3 healthy epithelium cell line PNT1A. cytotoxicity results showed that inhibited proliferation cells a dose-dependent manner. Compound 7a had highest toxic effect on colorectal carcinoma (IC50: 4.7 µM), IC50 values 18.5 µM 74.4 prostate lung cells, Furthermore, compound 4b found effective hepatocellular 210.2 µM). As result, can be developed treat cell. They considered as preliminary result for molecular-level research.