Design, Synthesis, and Mechanistic Investigations of Bile Acid–Tamoxifen Conjugates for Breast Cancer Therapy

摘要: We have synthesized two series of bile acid tamoxifen conjugates using three acids lithocholic (LCA), deoxycholic (DCA), and cholic (CA). These acid–tamoxifen possess 1, 2, 3 molecules attached to hydroxyl groups having free amine functionalities at the tail region acids. The in vitro anticancer activities these show that headgroup based conjugate (CA-Tam3-Am) is most potent as compared parent drug other conjugates. bearing shows enhanced both estrogen receptor +ve −ve breast cancer cell lines. activity CA-Tam3-Am due more favorable irreversible electrostatic interactions followed by intercalation co...