Loading...
Design, synthesis and evaluation of novel 16-imidazolyl substituted steroidal derivatives possessing potent diversified pharmacological properties.
Bansal, Ranju Guleria, Sheetal Thota, Sridhar Bodhankar, Subhash L Patwardhan, Moreshwar R Zimmer, Christina Hartmann, Rolf W Harvey, Alan L
Bansal, Ranju
Guleria, Sheetal
Thota, Sridhar
Bodhankar, Subhash L
Patwardhan, Moreshwar R
Zimmer, Christina
Hartmann, Rolf W
Harvey, Alan L
Citations
Altmetric:
Advisors
Editors
Other Contributors
Issue Date
2012-05
Submitted date
Files
Loading...
original manuscript
Adobe PDF, 368.21 KB
Other Titles
Abstract
As a part of our investigations into the structural-activity relationship studies of a novel class of medicinally active 16-substituted steroids, several new 16-imidazolyl substituted steroidal derivatives have been synthesized and pharmacologically evaluated in the current study. The new steroidal analogues 5, 6, 8, 9, 11 and 12 exhibited moderate cytotoxic effects in sixty cancer cell lines derived from nine cancers types. The imidazolyl substituted steroidal derivatives 6 (DPJ-RG-1241) and 7 (RB-401) were obtained as the powerful inhibitors of aromatase with IC50=0.18 μM and IC50=0.168 μM, respectively, approximately 1.2 and 1.4 times more potent in comparison to standard drug exemestane. The bis-quaternary steroids 13 and 14 displayed potent skeletal muscle relaxant properties. An affinity constant of 0.007 μM was observed for compound 14 on frog rectus abdominis muscle preparation and 13 displayed a very high anticholinesterase activity K(i)=25 nM, approximately 115-fold higher in comparison to standard drug galanthamine (K(i)=2.9 μM).
Citation
Design, synthesis and evaluation of novel 16-imidazolyl substituted steroidal derivatives possessing potent diversified pharmacological properties. 2012, 77 (6):621-9 Steroids
Publisher
Journal
PubMed ID
PubMed Central ID
Additional Links
Embedded video
Type
Article
Language
en
Description
Series/Report no.
ISSN
1878-5867
EISSN
ISBN
ISMN
Gov't Doc #
Sponsors
License
Archived with thanks to Steroids