Antiproliferative Properties of Vinyl Dipeptides: Synthesis and MCF-7 Cell Line Testing

• 作者: Ashraf Hassan Bayoumi
• 来源期刊: 药物化学期刊(英文)
• 学科: 医学
• 关键词: Piptidomimetics VINYL DIPEPTIDES 2-Aminopropenamide ANTIPROLIFERATIVE BREAST Cancer FURAN DERIVATIVES
• 年，卷（期）: 2012,（4）
• 页码范围: 105-111
• 页数: 7页
• 分类号: R73

摘要

Peptide mimics derived with close structure to peptide have vast utility because they are expected to interfere with biological targets while having superior drug-like properties if compared to peptides. In this work, novel vinyl dipeptides which are different in a double bond between the α-carbon of peptide and C1 of its side chain. Added to that, suitable substituents were selected to harness drug-like properties. The compounds were found to have moderate activities when tested against MCF-7 breast cancer cell line. For instance, the adamantyl analogue 2-(benzoylamino)-3-(2-furyl)-N-(1-adamantyl) propenamide (1c) and the heterocyclic analogue 2-(Benzoylamino)-3-(2-furyl)-N-[2-(5-cyanothia-zol-2-yl)] propenamide (1o) exhibited inhibition potency at 27.4 and 37.8 μM, respectively.