A number of uracil amides cleave poly (ADP-ribose) polymerase and therefore novel thiouracil amide compounds were synthesized and screened for the loss of cell viability in a human-estrogen-receptor-positive breast cancer cell line. The synthesized compounds exhibited moderate to significant efficacy against human breast cancer cells, where the compound 5e IC₅₀ value was found to be 18 μM. Thouracil amide compounds 5a and 5e inhibited the catalytical activity of PARP1, enhanced cleavage of PARP1, enhanced phosphorylation of H2AX, and increased CASPASE 3/7 activity. Finally, in silico analysis demonstrated that compound 5e interacted with PARP1. Hence, specific thiouracil amides may serve as new drug-seeds for the development of PARP inhibitors for use in oncology.

We herein report the preparation and characterization of an inexpensive polymer supported 1,3-bis(benzimidazolyl)benzeneCo(II) complex [PS-Co(BBZN)Cl₂] as a catalyst by using the polymer (divinylbenzene cross-linked chloromethylated polystyrene), on which 1,3-bis(benzimidazolyl)benzeneCo(II) complex (PS-Co(BBZN)Cl₂) has been immobilized. This catalyst was employed to develop arylamination reaction and robustness of the same reaction was demonstrated by synthesizing various bioactive adamantanyl-tethered-biphenylamines. Our synthetic methodology was much improved than reported methods due to the use of an inexpensive and recyclable catalyst.