Abstract 4491: Discovery of potent small molecular tubulin inhibitors for the treatment of cancer

Microtubule is a well-established drug target for the treatment of cancer. Drugs acting at this target include paclitaxel and docetaxel that stabilize the microtubules and prevent cancer cells from going through mitosis. These drugs are very successful chemotherapy agents and widely used for the treatment of cancer. In this presentation, we report the discovery of several series of novel and potent small molecular tubulin inhibitors and the identification of IMP03138 as a preclinical candidate. IMP03138 has advantages over the most commonly used anti-cancer drug paclitaxel in several in vitro assays and in vivo efficacy studies. Importantly, IMP03138 is highly effective against multi-drug resistant cancer cells. IMP3138 is currently undergoing IND enabling studies. Citation Format: Sui Xiong Cai, Zenghui Yu, Lei Chen, Qingbing Xu, Lizhen Wu, Lijun Liu, Feng Yin, Guoxiang Wang, Yangzhen Jiang, Xiuyan Zhang, Lingsheng Kong, Qingli Bao, Ye Edward Tian. Discovery of potent small molecular tubulin inhibitors for the treatment of cancer. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 4491. doi:10.1158/1538-7445.AM2013-4491