Natural steroids and their synthetic congeners were extensively studied during the last decade (1, 2). In a previous work, some new heterocyclic compounds showing antiparkinsonian (3), antitumor (4-6), antimicrobial (7-10) and anti-inflammatory (11) activity were synthesized. We found that certain substituted steroidal derivatives showed androgenic, anabolic and anti-inflammatory activities (12). Steroidal pyrazolines are an interesting group of compounds, many of which possess wide spread pharmacological properties such as analgesic, antipyretic and antiandrogenic activities (13,14). These derivatives are also well known for their pronounced anti-inflammatory (15) activity and are used as potent antidiabetic agents (16). In addition, the pharmacological and antitumor activities of many heterocyclic compounds have been reviewed (17)(18)(19). Recently, nitrogenous derivatives exhibited a general ionophoric potency for divalent cations (20) and are used as novel thiocyanate-selective membrane sensors (21). In view of these reports and in continuation of our previous work in heterocyclic chemistry, we have herein synthesized some new compounds containing steroidal structure for the evaluation of androgenic-anabolic activity as compared to testosterone as standard drug (Fig. 1). Accepted February 5, 2008 In this study, we synthesized some new substituted steroidal derivatives using 3b-hydroxyandrosten-17-one (dehydroepiandrosterone) as starting material. The synthesized steroidal derivatives 1-11 were evaluated for their androgenic-anabolic activities compared to testosterone as positive control. Details of the synthesis, spectroscopic data and toxicity (LD 50 ) of synthesized compounds are reported.