Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents

Publication date: August 2018Source: Steroids, Volume 136Author(s): Muafia Jabeen, Muhammad Iqbal Choudhry, Ghulam Abbas Miana, Khondaker Miraz Rahman, Umer Rashid, Hidayat-ullah Khan, Arshia, Abdul SadiqAbstractSteroidal hormones progesterone and testosterone play a vital role in breast and prostate cancers. In this research, we have synthesized and characterized a total of thirty-one (31) new nitrogenous derivatives of progesterone and testosterone. The synthesized derivatives (1–31) were screened for their anti-cancer potential against MCF-7 and PC-3 cell lines of breast using MTT assay. The compounds 1-31exhibited significant inhibitory potentials against MCF-7 and PC-3 cell lines. In MCF-7 assay, compound 17 displayed IC50 value of 04 ± 0.02 μM while compound 18 was leading in PC-3 assay with IC50 of 03.14 ± 0.4 μM. Tamoxifen was used as positive control which exhibited an IC50of 0.12 ± 0.03 and 0.26 ± 0.01 μM against MCF-7 and PC-3 respectively. The compounds also showed good anti-inflammatory activity according to oxidative burst inhibition by chemiluminescence technique where ibuprofen was used as positive control with 73.2 ± 1.4% ROS inhibition. The compounds showed the percent ROS inhibition between 23.2 ± 0.2 and −3.2 ± 4.1. The results of the compounds were compared with the positive control ibuprofen. Molecular docking correlations suggest that the compounds exerted their inhibitory activity by binding to the active...
Source: Steroids - Category: Drugs & Pharmacology Source Type: research