Synthesis and biological activity of novel 3'-trifluoromethyl taxoids

Iwao Ojima; John C. Slater; Paula Pera; Jean M. Veith; Ahmed Abouabdellah; Jean Pierre Bégué; Ralph J. Bernacki

doi:10.1016/S0960-894X(96)00595-1

Synthesis and biological activity of novel 3'-trifluoromethyl taxoids

Iwao Ojima
, John C. Slater
, Paula Pera
, Jean M. Veith
, Ahmed Abouabdellah
, Jean Pierre Bégué
, Ralph J. Bernacki

Chemistry

Stony Brook University

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

47 Scopus citations

Abstract

Second generation taxoids possessing a trifluoromethyl moiety in place of the 3'-phenyl group are synthesized by means of the β-Lactam Synthon Method. The in vitro cytotoxicities of these new taxoids are evaluated against several different human cancer cell lines and found to exhibit greatly enhanced activities as compared to those of paclitaxel and docetaxel. The activity enhancement is most remarkable against a drug resistant breast cancer cell line, MCF7-R, expressing MDR phenotype.

Original language	English
Pages (from-to)	133-138
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	7
Issue number	2
DOIs	https://doi.org/10.1016/S0960-894X(96)00595-1
State	Published - Jan 21 1997

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title = "Synthesis and biological activity of novel 3'-trifluoromethyl taxoids",

abstract = "Second generation taxoids possessing a trifluoromethyl moiety in place of the 3'-phenyl group are synthesized by means of the β-Lactam Synthon Method. The in vitro cytotoxicities of these new taxoids are evaluated against several different human cancer cell lines and found to exhibit greatly enhanced activities as compared to those of paclitaxel and docetaxel. The activity enhancement is most remarkable against a drug resistant breast cancer cell line, MCF7-R, expressing MDR phenotype.",

author = "Iwao Ojima and Slater, \{John C.\} and Paula Pera and Veith, \{Jean M.\} and Ahmed Abouabdellah and B{\'e}gu{\'e}, \{Jean Pierre\} and Bernacki, \{Ralph J.\}",

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T1 - Synthesis and biological activity of novel 3'-trifluoromethyl taxoids

AU - Ojima, Iwao

AU - Slater, John C.

AU - Pera, Paula

AU - Veith, Jean M.

AU - Abouabdellah, Ahmed

AU - Bégué, Jean Pierre

AU - Bernacki, Ralph J.

PY - 1997/1/21

Y1 - 1997/1/21

N2 - Second generation taxoids possessing a trifluoromethyl moiety in place of the 3'-phenyl group are synthesized by means of the β-Lactam Synthon Method. The in vitro cytotoxicities of these new taxoids are evaluated against several different human cancer cell lines and found to exhibit greatly enhanced activities as compared to those of paclitaxel and docetaxel. The activity enhancement is most remarkable against a drug resistant breast cancer cell line, MCF7-R, expressing MDR phenotype.

AB - Second generation taxoids possessing a trifluoromethyl moiety in place of the 3'-phenyl group are synthesized by means of the β-Lactam Synthon Method. The in vitro cytotoxicities of these new taxoids are evaluated against several different human cancer cell lines and found to exhibit greatly enhanced activities as compared to those of paclitaxel and docetaxel. The activity enhancement is most remarkable against a drug resistant breast cancer cell line, MCF7-R, expressing MDR phenotype.

UR - https://www.scopus.com/pages/publications/0031023523

U2 - 10.1016/S0960-894X(96)00595-1

DO - 10.1016/S0960-894X(96)00595-1

M3 - Article

SN - 0960-894X

VL - 7

SP - 133

EP - 138

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Synthesis and biological activity of novel 3'-trifluoromethyl taxoids

Abstract

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