Synthesis and Antiproliferative Activities of Triphenylmethanol Conjugates of Leuprorelin

• 作者: Jawzah Alnakhli Kaleh Karim Ryan Beni Samiyah Alhamed William Boadi
• 来源期刊: 药物化学期刊(英文)
• 学科: 医学
• 关键词: PRODRUGS LEUPRORELIN POLYPHENOLS PROSTATE Cancer Triphenylmethanol
• 年，卷（期）: 2019,（2）
• 页码范围: 37-47
• 页数: 11页
• 分类号: R73

摘要

Leuprorelin®(LEP) is an FDA drug for breast cancer and prostate cancer treatment. There are several reported adverse effects such as transient hypertension, excessive salivation, and increased dysuria during treatment with LEP. In this study, the efficacy and toxicity of LEP were modified by using a drug delivery system to adjust the physicochemical properties. In this regard, Leuprorelin®conjugates of triphenylmethanol derivatives (TPMs) were synthesized as prodrugs. Comparative antiproliferative assays showed that LEP-TPMs conjugates had significantly higher antiproliferative activities than the corresponding non-covalent physical mixtures of the TPMs and LEP against human invasive ductal carcinoma (BT-549), human prostate carcinoma (PC3), human lung cancer (A549) and mouse pre-adipocytes (3T3-L1) cells.