Synthesis and structure-activity relationships of new second-generation taxoids

Iwao Ojima; Tao Wang; Michael L. Miller; Songnian Lin; Christopher P. Borella; Xudong Geng; Paula Pera; Ralph J. Bernacki

doi:10.1016/S0960-894X(99)00629-0

Synthesis and structure-activity relationships of new second-generation taxoids

Iwao Ojima
, Tao Wang
, Michael L. Miller
, Songnian Lin
, Christopher P. Borella
, Xudong Geng
, Paula Pera
, Ralph J. Bernacki

Chemistry

Stony Brook University
Roswell Park Cancer Institute

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

91 Scopus citations

Abstract

A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as 'advanced second generation taxoids'.

Original language	English
Pages (from-to)	3423-3428
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	9
Issue number	24
DOIs	https://doi.org/10.1016/S0960-894X(99)00629-0
State	Published - Dec 20 1999

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title = "Synthesis and structure-activity relationships of new second-generation taxoids",

abstract = "A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as 'advanced second generation taxoids'.",

author = "Iwao Ojima and Tao Wang and Miller, \{Michael L.\} and Songnian Lin and Borella, \{Christopher P.\} and Xudong Geng and Paula Pera and Bernacki, \{Ralph J.\}",

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T1 - Synthesis and structure-activity relationships of new second-generation taxoids

AU - Ojima, Iwao

AU - Wang, Tao

AU - Miller, Michael L.

AU - Lin, Songnian

AU - Borella, Christopher P.

AU - Geng, Xudong

AU - Pera, Paula

AU - Bernacki, Ralph J.

PY - 1999/12/20

Y1 - 1999/12/20

N2 - A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as 'advanced second generation taxoids'.

AB - A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as 'advanced second generation taxoids'.

UR - https://www.scopus.com/pages/publications/0033590281

U2 - 10.1016/S0960-894X(99)00629-0

DO - 10.1016/S0960-894X(99)00629-0

M3 - Article

C2 - 10617084

AN - SCOPUS:0033590281

SN - 0960-894X

VL - 9

SP - 3423

EP - 3428

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Synthesis and structure-activity relationships of new second-generation taxoids

Abstract

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