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Structure-activity relationship (SAR)of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads

Tipo de material: TextoTextoSeries ; Bioorganic & Medicinal Chemistry Letters, 19(15), p.4394-4398, 2009Trabajos contenidos:
  • Shah, B.A
  • Kaur, R
  • Gupta, P
  • Kumar, A
  • Sethi, V.K
  • Andotra, S.S
  • Singh, J
  • Singh, J
  • Taneja, S.C
Tema(s): Recursos en línea: Resumen: Analogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure-activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa)and human myeloid leukemia (HL-60)cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II.
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Analogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure-activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa)and human myeloid leukemia (HL-60)cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II.

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