Drug Res (Stuttg) 2018; 68(02): 100-103
DOI: 10.1055/s-0043-118538
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Hybrids of Steroid and Nitrogen Mustard as Antiproliferative Agents: Synthesis, In Vitro Evaluation and In Silico Inverse Screening

Pratap Chandra Acharya
1   University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India
,
Ranju Bansal
1   University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India
,
Prashant S. Kharkar
2   Department of Pharmaceutical Chemistry, SPP School of Pharmacy and Technology Management, SVKM’S NMIMS, Mumbai, India
› Author Affiliations
Further Information

Publication History

received 19 June 2017

accepted 13 August 2017

Publication Date:
26 September 2017 (online)

Abstract

Hybrids of 16E-arylidene steroids and nitrogen mustard have been synthesized and evaluated for their in vitro cytotoxic activity to develop tissue specific antineoplastic agents from steroids. These hybrids displayed specificity towards leukemia cell lines, however somewhat reduced potency was observed in comparison with the earlier reported 16E-arylidene steroids. The in silico reverse screening experiments were employed to find out the probable pharmacological mechanism of these hybrids. Molecular docking studies suggested glucocorticoid receptors as a probable target for the antileukemic action of these steroid-nitrogen mustard hybrids.

Supplementary Material

 
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