Insights into podophyllotoxin lactone features: New cyclolignans as potential dual tubulin‐topoisomerase II inhibitors DOI Creative Commons
Ángela‐Patricia Hernández,

Celia Rosales‐Fernández,

Carolina Miranda‐Vera

и другие.

Archiv der Pharmazie, Год журнала: 2024, Номер 358(1)

Опубликована: Ноя. 12, 2024

Abstract Chemomodulation of natural cyclolignans as podophyllotoxin has been a successful approach to obtain semisynthetic bioactive derivates. One example this is the FDA‐approved drug etoposide for solid and hematological tumors. It differs from antimitotic activity product in its mechanism action, being topoisomerase II inhibitor instead tubulin antimitotic. Within molecular requirements these compounds, trans‐γ‐lactone moiety presented parent compound always feature be explored chemomodulate bioactivity. In study, we have obtained different compounds that comply with characteristics antitubulin antitopoisomerase combined single molecule. Furthermore, influence trans ‐lactone on final activity, finding cis was also interesting terms The best values cytotoxicity cell cycle inhibition were lacking lactone ring, thus mimicking podophyllic aldehyde functionalization, selective derivate. analogs cytotoxic activity. present study illustrates potential chemomodulation products such cyclolignan derivates discovery new antitumor agents.

Язык: Английский

Insights into podophyllotoxin lactone features: New cyclolignans as potential dual tubulin‐topoisomerase II inhibitors DOI Creative Commons
Ángela‐Patricia Hernández,

Celia Rosales‐Fernández,

Carolina Miranda‐Vera

и другие.

Archiv der Pharmazie, Год журнала: 2024, Номер 358(1)

Опубликована: Ноя. 12, 2024

Abstract Chemomodulation of natural cyclolignans as podophyllotoxin has been a successful approach to obtain semisynthetic bioactive derivates. One example this is the FDA‐approved drug etoposide for solid and hematological tumors. It differs from antimitotic activity product in its mechanism action, being topoisomerase II inhibitor instead tubulin antimitotic. Within molecular requirements these compounds, trans‐γ‐lactone moiety presented parent compound always feature be explored chemomodulate bioactivity. In study, we have obtained different compounds that comply with characteristics antitubulin antitopoisomerase combined single molecule. Furthermore, influence trans ‐lactone on final activity, finding cis was also interesting terms The best values cytotoxicity cell cycle inhibition were lacking lactone ring, thus mimicking podophyllic aldehyde functionalization, selective derivate. analogs cytotoxic activity. present study illustrates potential chemomodulation products such cyclolignan derivates discovery new antitumor agents.

Язык: Английский

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