Synthesis and biological evaluation of chalcone-polyamine conjugates as novel vectorized agents in colorectal and prostate cancer chemotherapy

The aim of this study was to synthesize chalcone-polyamine conjugates in order enhance bioavailability and selectivity chalcone core towards cancer cells, using polyamine-based vectors. Indeed, it is well-known that polyamine transport system upregulated tumor cells. 3′,4,4′,5′-tetramethoxychalcone selected as parent since found be an efficient anti-proliferative agent on various A series five obtained the 4-bromopropyloxy-3′,4′,5′-trimethoxychalcone a key intermediate. Chalcone tails were fused through amine bond. These possess marked vitro antiproliferative effect against colorectal (HT-29 HCT-116) prostate (PC-3 DU-145) cell lines. most active conjugate (compound 8b) then chosen for further biological evaluations elucidate mechanisms responsible its activity. Investigations cycle distribution revealed can prevent proliferation human cells by blocking at G1 G2 phase, respectively. Flow cytometry analysis sub-G1 peak, characteristic apoptotic population our inquiries highlighted apoptosis induction early later stages several pro-apoptotic markers. Therefore, chalcone-N1-spermidine could considered promising colon prostatic adjuvant therapy.