본문 바로가기
HOME> 논문 > 논문 검색상세

논문 상세정보

European journal of medicinal chemistry v.143, 2018년, pp.732 - 744   SCI SCIE
본 등재정보는 저널의 등재정보를 참고하여 보여주는 베타서비스로 정확한 논문의 등재여부는 등재기관에 확인하시기 바랍니다.

O2-(2,4-dinitrophenyl)diazeniumdiolates derivatives: Design, synthesis, cytotoxic evaluation and reversing MDR in MCF-7/ADR cells

Li, Qixing (Corresponding author. ) ; Zou, Pian (Corresponding author. ) ; Sun, Jianbo ; Chen, Li ;
  • 초록  

    Abstract A series of O 2 -(2,4-dinitrophenyl)diazeniumdiolates derivatives were designed, synthesized and antiproliferative activities evaluated as novel nitric oxide (NO)-releasing prodrugs that could be activated by glutathione S-transferases π (GSTπ). Most of these derivatives exhibited significant antiproliferative activities compared to the reported NO-donor prodrug JS-K, among which compounds 27 and 36 had superior potency with IC 50 below 1 μM. NO released amounts detection of all derivatives indicated that the antiproliferative activities were positively correlated with the levels of intracellular NO release in HCT116 cells. The most potent compound 36 exhibited improved uncatalyzed stability of GSTπ. Additionally, 36 showed remarkably multidrug resistance reversal activity which reversed multidrug resistance of adriamycin (ADR) in MCF-7/ADR cells with IC 50 from 84.94 μM to 1.13 μM. Highlights A series of diazeniumdiolates derivatives were designed and synthesized. Most of the derivatives exhibited significant cytotoxicities compared to JS-K. The cytotoxicities positively correlated with the amounts of NO release in HCT116. The most potent compound 36 exhibited improved uncatalyzed stability of GSTπ. Compound 36 also showed remarkably multidrug resistance reversal activity. Graphical abstract A series of O 2 -(2,4-dinitrophenyl) diazeniumdiolates derivatives were designed, synthesized and antiproliferative activities evaluated as novel nitric oxide (NO)-releasing prodrugs that could be activated by glutathione S-transferases π (GSTπ). Compound 36 showed remarkably multidrug resistance reversal activity which reversed multidrug resistance of adriamycin (ADR) in MCF-7/ADR cells. [DISPLAY OMISSION]


  • 주제어

    Diazeniumdiolates .   No-Releasing .   JS-K .   Adriamycin .   Multidrug resistance.  

 활용도 분석

  • 상세보기

    amChart 영역
  • 원문보기

    amChart 영역

원문보기

무료다운로드
  • 원문이 없습니다.

유료 다운로드의 경우 해당 사이트의 정책에 따라 신규 회원가입, 로그인, 유료 구매 등이 필요할 수 있습니다. 해당 사이트에서 발생하는 귀하의 모든 정보활동은 NDSL의 서비스 정책과 무관합니다.

원문복사신청을 하시면, 일부 해외 인쇄학술지의 경우 외국학술지지원센터(FRIC)에서
무료 원문복사 서비스를 제공합니다.

NDSL에서는 해당 원문을 복사서비스하고 있습니다. 위의 원문복사신청 또는 장바구니 담기를 통하여 원문복사서비스 이용이 가능합니다.

이 논문과 함께 출판된 논문 + 더보기