The invention provides di-peptide conjugated antitumor agents, pharmaceutical compositions and methods for preparation and use thereof for treating various cancer and inflammation-related diseases and conditions. The present invention addresses the shortcomings of the existing anti-tumor and anti-inflammatory drugs, particularly in that the anti-tumor agents of the invention that selectively kill cancer cells with minimal damage to normal cells. Similarly, the anti-inflammatory agents of the invention provide effective treatment of various inflammatory diseases and conditions without the many deleterious side effects commonly associated with steroids
