We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC...We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC-MS/MS analytical method for one of the lead novel anticancer makaluvamine analog,TCBA-TPQ,and conducted a pharmacokinetic study in laboratory rats.Our results indicated that the HPLC-MS/MS method was precise,accurate,and specific.Using this method,we carried out in vitro and in vivo evaluations of the pharmacological properties of TCBA-TPQ and plasma pharmacokinetics in rats.Our results provide a basis for future preclinical and clinical development of this promising anticancer marine analog.展开更多
基金supported by the National Institutes of Health(NIH)grants R01 CA112029,R01 CA121211,and R01 CA186662(to R.Z.)and 1UL1RR025777(to S.V.)
文摘We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC-MS/MS analytical method for one of the lead novel anticancer makaluvamine analog,TCBA-TPQ,and conducted a pharmacokinetic study in laboratory rats.Our results indicated that the HPLC-MS/MS method was precise,accurate,and specific.Using this method,we carried out in vitro and in vivo evaluations of the pharmacological properties of TCBA-TPQ and plasma pharmacokinetics in rats.Our results provide a basis for future preclinical and clinical development of this promising anticancer marine analog.
