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

Bansal, Ranju; Acharya, Pratap Chandra

doi:10.1016/j.steroids.2012.01.020

Cited by 18 publications

(15 citation statements)

References 16 publications

(23 reference statements)

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“…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.…”

Section: Introductionmentioning

confidence: 99%

“…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.…”

Section: Introductionmentioning

confidence: 99%

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

2017

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Hybrids of 16E-arylidene steroids and nitrogen mustard have been synthesized and evaluated for their in vitro cytotoxic activity to develop tissue specific antineoplastic agents from steroids. These hybrids displayed specificity towards leukemia cell lines, however somewhat reduced potency was observed in comparison with the earlier reported 16E-arylidene steroids. The in silico reverse screening experiments were employed to find out the probable pharmacological mechanism of these hybrids. Molecular docking studies suggested glucocorticoid receptors as a probable target for the antileukemic action of these steroid-nitrogen mustard hybrids.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

2017

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“…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.…”

Section: Introductionmentioning

confidence: 99%

Recent syntheses of steroidal oxazoles, oxazolines and oxazolidines

Bendif¹,

Ibrahim‐Ouali²,

Dumur³

2021

Arkivoc

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“…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.…”

Section: Introductionmentioning

confidence: 99%