Studies on novel D-ring substituted steroidal pyrazolines as potential anticancer agents

Studies on novel D-ring substituted steroidal pyrazolines as potential anticancer agents

An efficient and facile synthesis of 17-pyrazolinyl derivatives of pregnenolone and their evaluation as potential anticancer agents against various human cancer cell lines are reported. The scheme involves the transformation of the starting pregnenolone acetate into pregnenolone, conversion of pregn...

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Bibliographic Details
Published in:Steroids Vol. 75; no. 12; pp. 805 - 809
Main Authors: Banday, Abid H., Mir, Bilal P., Lone, Imtiyaz H., Suri, K.A., Kumar, H.M. Sampath
Format: Journal Article
Language:English
Published: Kidlington Elsevier Inc 01-12-2010
Elsevier
Subjects:
Aldehydes - chemistry
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Benzylidene Compounds - chemistry
Benzylidines
Biological and medical sciences
Cell Line, Tumor
Dipolar cycloaddition
Fundamental and applied biological sciences. Psychology
Humans
Pregnenolone
Pregnenolone - analogs & derivatives
Pregnenolone - chemical synthesis
Pregnenolone - pharmacology
Pyrazoles - chemistry
Pyrazoline
Vertebrates: endocrinology
Benzylidines
Pyrazoline
Pregnenolone
Dipolar cycloaddition
Antineoplastic agent
Corticosteroid
Adrenal hormone
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Summary:An efficient and facile synthesis of 17-pyrazolinyl derivatives of pregnenolone and their evaluation as potential anticancer agents against various human cancer cell lines are reported. The scheme involves the transformation of the starting pregnenolone acetate into pregnenolone, conversion of pregnenolone to the corresponding benzylidine derivatives and finally the conversion of this derivative to the stable steroidal 17-pyrazoline. Various compounds 4b, 4c, 4e, 4f, 4h and 4j showed significant cytotoxic activity especially against HT-29, HCT-15, 502713 cell lines.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0039-128X
1878-5867
DOI:10.1016/j.steroids.2010.02.014