Comprehensive Study of Sansalvamide A Derivatives and their Structure–Activity Relationships against Drug-Resistant Colon Cancer Cell Lines
Citations Over TimeTop 10% of 2008 papers
Abstract
We report an extensive structure-activity relationship (SAR) of 62 compounds active against two drug-resistant colon cancer cell lines. Our comprehensive evaluation of two generations of compounds utilizes SAR, NMR, and molecular modeling to evaluate the key 3D features of potent compounds. Of the seven most potent compounds reported here, five are second-generation, emphasizing our ability to incorporate potent features found in the first generation and utilize their structures to design potency into the second generation. These analogs share no structural homology to current colon cancer drugs, are cytotoxic at levels on par with existing drugs treating other cancers, and demonstrate selectivity for drug-resistant colon cancer cell lines over noncancerous cell lines. Thus, we have established sansalvamide A as an excellent lead for treating multiple drug-resistant colon cancers.
Related Papers
- → Establishment of a Potency Test by ELISA for a Rabies Vaccine for Animal Use in Japan(2003)15 cited
- → Quantitative Structure-Activity Relationships of 5-Lipoxygenase Inhibitors. Inhibitory Potency of Pyridazinone Analogues(1994)13 cited
- → ICR Expands CanSAR Drug Discovery Platform(2013)1 cited
- → The Experimental Study on the continuous Anti-bacterial Potency of Coptidis rhizoma extract on Cultivation of Staphylococcus species(S. aureus, S. epidermidis)(2007)1 cited
- → Potency analysis of cellular therapies: the role of molecular assays(2021)