3 years ago

In pursuit of balgacyclamide A – Discovery of an oxazoline macrocycle with multiple myeloma cytotoxicity and penetration

In pursuit of balgacyclamide A – Discovery of an oxazoline macrocycle with multiple myeloma cytotoxicity and penetration
Four new oxazoline based macrocycles have been constructed, said cycles were found to possess varying cytotoxicity against six different cancer cell lines: IC50 values of 6.4μM towards HeLa and 11.9μM towards LnCaP being the most potent. Two of the four macrocycles were found to have marginal cytotoxicity against MM.1S and MM.1R, myeloma cancer cell lines, and further evaluation showed that they also possessed rapid cellular uptake and accumulation characteristics. Through the structure-activity relationship comparisons between the four compounds, it was found that the C6 position of the E-ring is amendable to substitution and could possibly serve as a conjugation site for the development of a selective delivery system to MM.1R.

Publisher URL: www.sciencedirect.com/science

DOI: S0040403917312078

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