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

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

doi:10.1016/S0968-0896(00)00093-6

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

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

Chemistry

Stony Brook University
Roswell Park Cancer Institute
Catholic University of the Sacred Heart

Research output: Contribution to journal › Article › peer-review

52 Scopus citations

Abstract

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. Copyright (C) 2000 Elsevier Science Ltd.

Original language	English
Pages (from-to)	1619-1628
Number of pages	10
Journal	Bioorganic and Medicinal Chemistry
Volume	8
Issue number	7
DOIs	https://doi.org/10.1016/S0968-0896(00)00093-6
State	Published - Jul 2000

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10.1016/S0968-0896(00)00093-6

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title = "Syntheses and biological activity of C-3'-difluoromethyl-taxoids",

abstract = "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. Copyright (C) 2000 Elsevier Science Ltd.",

author = "Iwao Ojima and Songnian Lin and Slater, \{John C.\} and Tao Wang and Paula Pera and Bernacki, \{Ralph J.\} and Cristiano Ferlini and Giovanni Scambia",

year = "2000",

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AU - Ojima, Iwao

AU - Lin, Songnian

AU - Slater, John C.

AU - Wang, Tao

AU - Pera, Paula

AU - Bernacki, Ralph J.

AU - Ferlini, Cristiano

AU - Scambia, Giovanni

PY - 2000/7

Y1 - 2000/7

N2 - 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. Copyright (C) 2000 Elsevier Science Ltd.

AB - 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. Copyright (C) 2000 Elsevier Science Ltd.

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DO - 10.1016/S0968-0896(00)00093-6

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AN - SCOPUS:0033948409

SN - 0968-0896

VL - 8

SP - 1619

EP - 1628

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 7

ER -

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

Abstract

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