Suresha, N. and Metri, Prashant K. and Rashmi, S. and Yang, Ji-Rui and Shobith, R. and Swamynayaka, Ananda and Shanmugam, Muthu K. and Nagaraja, Omantheswara and Madegowda, Mahendra and Babu Shubha, Priya and Chinnathambi, Arunachalam and Alharbi, Sulaiman Ali and Pandey, Vijay and Ahn, Kwang Seok and Lobie, Peter E. and Basappa, B. (2022) Development of 1-(4-(Substituted)piperazin-1-yl)-2-((2-((4-methoxybenzyl)thio)pyrimidin-4-yl)oxy)ethanones That Target Poly (ADP-Ribose) Polymerase in Human Breast Cancer Cells. Molecules, 27 (9). ISSN 1420-3049
Full text not available from this repository. (Request a copy)Abstract
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.
| Item Type: | Article |
|---|---|
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | C Swapna Library Assistant |
| Date Deposited: | 17 Jun 2023 05:25 |
| Last Modified: | 17 Jun 2023 05:25 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/17547 |
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