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The main objective of the present work is description of design, synthesis and characterisation of cholesteryl pyrazolines along with their antitumor studies against human tumor cell lines. The identity of the newly synthesized compounds has been ascertained by IR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. The First chapter contains introduction regarding importance of cancer, applications of steroids as antitumor agents and biological utility of pyrazoline derivatives. The second and third chapters deal with the synthesis, characterization and stereochemical aspects of steroidal pyrazolines while fourth chapter embodies antitumor evaluation of the newly synthesized compounds.