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Syntheses and biological activity of C-3′-difluoromethyl-taxoids

Ojima, Iwao ; Lin, Songnian ; Slater, John C ; Wang, Tao ; Pera, Paula ; Bernacki, Ralph J ; Ferlini, Cristiano ; Scambia, Giovanni

Bioorganic & Medicinal Chemistry, July 2000, Vol.8(7), pp.1619-1628 [Peer Reviewed Journal]

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  • Title:
    Syntheses and biological activity of C-3′-difluoromethyl-taxoids
  • Author: Ojima, Iwao ; Lin, Songnian ; Slater, John C ; Wang, Tao ; Pera, Paula ; Bernacki, Ralph J ; Ferlini, Cristiano ; Scambia, Giovanni
  • Description: A series of new taxoids bearing difluoromethyl group at the C-3' position and modifications at the C-10 and C-14 positions has been synthesized and their biological activities studied. The in vitro cytotoxicity assay results indicate that these newly developed taxoids exhibit comparable to several times better activity against drug-sensitive cell line LCC6-WT, and 40-70 times better activity against the corresponding drug-resistant cancer cell line LCC6-MDR as compared to that of paclitaxel. Apoptosis analysis has revealed the exceptional activity of SB-T-12843 (1e) in inducing apoptosis in both MDR-bearing and MDR-negative cancer cells.
  • Is Part Of: Bioorganic & Medicinal Chemistry, July 2000, Vol.8(7), pp.1619-1628
  • Identifier: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/S0968-0896(00)00093-6
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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