Synthesis and antileukemic activity of 16E-[4-(2-carboxy)ethoxybenzylidene]-androstene amides

Hybrids of Steroid and Nitrogen Mustard as Antiproliferative Agents: Synthesis, In Vitro Evaluation and In Silico Inverse Screening

“…The failure of conventional chemotherapeutic agents to yield anticipated results in most of the cases has compelled to discover innovative agents with cancer selectivity [1]. Several 16E-arylidene androstene derivatives with varying degree of antineoplastic activity have been reported from our laboratory [2,3]. Our previous studies indicate that changing the substituents at C 16 of the steroid skeleton can generate tissue selective anticancer compounds.…”

“…Our previous studies indicate that changing the substituents at C 16 of the steroid skeleton can generate tissue selective anticancer compounds. Presence of tertiary amino groups through a 16-arylidene group at the C 16 position as well as replacement or substitution of C 3 -OH function has a prominent impact on potency as well as selectivity of this class of cytotoxic steroids [2]. The molecular hybridization strategy, in which pharmacologically crucial structural elements from two prototype molecules are combined to produce a non-identical twin drug, is employed as a rational drug design approach.…”

Recent syntheses of steroidal oxazoles, oxazolines and oxazolidines

“…It was found that introducing heterocycles into steroids, [7][8][9][10][11][12] by modification of the steroidal side chain or substitution of the steroidal skeleton, can result in a change in its biological activities. [13][14][15][16][17] Steroids containing heteroatoms have been widely researched and reported.…”

Recent syntheses of steroidal derivatives containing heterocycles

“…It was found that introducing heterocycles into steroids, [7][8][9][10][11][12] by modification of the steroidal side chain or substitution of the steroidal skeleton, introducing a heteroatom or replacing one or more carbon atoms in steroidal molecule with a heteroatom, can result in a change in its biological activities. [13][14][15][16][17] Steroids containing heteroatoms have been widely researched and reported.…”