King's College London

Research portal

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

Research output: Contribution to journalArticle

Standard

Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents. / Jabeen, Muafia; Choudhry, Muhammad Iqbal; Miana, Ghulam Abbas; Rahman, Khondaker Miraz; Rashid, Umer; Khan, Hidayat-ullah; Seddigh, Arshia; Sadiq, Abdul.

In: Steroids, Vol. 136, 08.2018, p. 22-31.

Research output: Contribution to journalArticle

Harvard

Jabeen, M, Choudhry, MI, Miana, GA, Rahman, KM, Rashid, U, Khan, H, Seddigh, A & Sadiq, A 2018, 'Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents', Steroids, vol. 136, pp. 22-31. https://doi.org/10.1016/j.steroids.2018.05.008

APA

Jabeen, M., Choudhry, M. I., Miana, G. A., Rahman, K. M., Rashid, U., Khan, H., Seddigh, A., & Sadiq, A. (2018). Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents. Steroids, 136, 22-31. https://doi.org/10.1016/j.steroids.2018.05.008

Vancouver

Jabeen M, Choudhry MI, Miana GA, Rahman KM, Rashid U, Khan H et al. Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents. Steroids. 2018 Aug;136:22-31. https://doi.org/10.1016/j.steroids.2018.05.008

Author

Jabeen, Muafia ; Choudhry, Muhammad Iqbal ; Miana, Ghulam Abbas ; Rahman, Khondaker Miraz ; Rashid, Umer ; Khan, Hidayat-ullah ; Seddigh, Arshia ; Sadiq, Abdul. / Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents. In: Steroids. 2018 ; Vol. 136. pp. 22-31.

Bibtex Download

@article{79efe572cc454f73af096f91ab913f1e,
title = "Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents",
abstract = "Steroidal 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 of the enzyme.",
keywords = "Progresterone, Testosterone, MTT assay, Anti-inflammatory, Molecular docking",
author = "Muafia Jabeen and Choudhry, {Muhammad Iqbal} and Miana, {Ghulam Abbas} and Rahman, {Khondaker Miraz} and Umer Rashid and Hidayat-ullah Khan and Arshia Seddigh and Abdul Sadiq",
year = "2018",
month = aug,
doi = "10.1016/j.steroids.2018.05.008",
language = "English",
volume = "136",
pages = "22--31",
journal = "Steroids",
issn = "0039-128X",
publisher = "Elsevier Inc.",

}

RIS (suitable for import to EndNote) Download

TY - JOUR

T1 - Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents

AU - Jabeen, Muafia

AU - Choudhry, Muhammad Iqbal

AU - Miana, Ghulam Abbas

AU - Rahman, Khondaker Miraz

AU - Rashid, Umer

AU - Khan, Hidayat-ullah

AU - Seddigh, Arshia

AU - Sadiq, Abdul

PY - 2018/8

Y1 - 2018/8

N2 - Steroidal 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 of the enzyme.

AB - Steroidal 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 of the enzyme.

KW - Progresterone

KW - Testosterone

KW - MTT assay

KW - Anti-inflammatory

KW - Molecular docking

U2 - 10.1016/j.steroids.2018.05.008

DO - 10.1016/j.steroids.2018.05.008

M3 - Article

VL - 136

SP - 22

EP - 31

JO - Steroids

JF - Steroids

SN - 0039-128X

ER -

View graph of relations

© 2020 King's College London | Strand | London WC2R 2LS | England | United Kingdom | Tel +44 (0)20 7836 5454