Anti-tumor activity of N-thiolated β-lactam antibiotics

作者：Chen, Di; Falsetti, Samuel C.; Frezza, Michael; Milacic, Vesna; Kazi, Aslamuzzaman; Cui, Qiuzhi Cindy; Long, Timothy E.; Turos, Edward; Dou, Q. Ping^*

来源：Cancer Letters, 2008, 268(1): 63-69.

DOI：10.1016/j.canlet.2008.03.047

• beta-lactam
• DNA damage
• apoptosis
• anti-tumor activity
• breast cancer

An ongoing strategy for cancer treatment is selective induction of apoptosis in cancer over normal cells. N-thiolated beta-lactams were found to induce DNA damage, growth arrest and apoptosis in cultured human cancer cells. However, whether these compounds have a similar effect in vivo has not been studied. We report here that treatment with the P-lactam L-1 caused a significant inhibition of tumor growth in a breast cancer xenograft mouse model, associated with induction of DNA damage and apoptosis in vivo. These results suggest that the synthetic antibiotic N-thiolated beta-lactams hold great potential to be developed as novel anti-cancer drugs. Published by Elsevier Ltd.

• 出版日期2008-9-8