Abstract
Several steroids (abiraterone, prednisone, testosterone, cholesterol) and the BCL-2 inhibitor bexarotene were used as starting materials to synthesize iperazinyl-spacered rhodamine B conjugates. The conjugates were screened for their cytotoxicity in SRB assays against several human tumor cell lines and found to be active in a low μM to nM range. The conjugate derived from testosterone held an EC50 = 59 nM against MCF-7 tumor cells and acted mainly by necrosis. The prednisone conjugate, however, was less cytotoxic but acted mainly by apoptosis and held a moderate selectivity against MCF-7 tumor cells.
Keywords:
Apoptosis; Cytotoxicity; Prednisone; Rhodamine B; Steroids; Synthesis.
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
MeSH terms
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Androstenes / chemical synthesis
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Androstenes / chemistry
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Androstenes / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects*
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Bexarotene / chemical synthesis
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Bexarotene / chemistry
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Bexarotene / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Cholesterol / chemical synthesis
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Cholesterol / chemistry
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Cholesterol / pharmacology
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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Mitochondria / drug effects*
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Molecular Structure
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Prednisone / chemical synthesis
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Prednisone / chemistry
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Prednisone / pharmacology
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Rhodamines / chemical synthesis
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Rhodamines / chemistry
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Rhodamines / pharmacology
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Structure-Activity Relationship
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Testosterone / chemical synthesis
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Testosterone / chemistry
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Testosterone / pharmacology
Substances
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Androstenes
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Antineoplastic Agents
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Rhodamines
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Testosterone
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Cholesterol
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Bexarotene
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abiraterone
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rhodamine B
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Prednisone