Synthesis of biologically active 2-benzoyl paclitaxel analogues

Gunda I. Georg; Syed M. Ali; Thomas C. Boge; Apurba Datta; Lise Falborg; Haeil Park; Marisan Mejillano; Richard H. Himes

doi:10.1016/0960-894X(95)00020-T

Synthesis of biologically active 2-benzoyl paclitaxel analogues

Gunda I. Georg, Syed M. Ali, Thomas C. Boge, Apurba Datta, Lise Falborg, Haeil Park, Marisan Mejillano, Richard H. Himes

Medicinal Chemistry

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Abstract

The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma cells. Most of the analogues were found to possess biological properties similar to paclitaxel.

Original language	English (US)
Pages (from-to)	259-264
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	5
Issue number	3
DOIs	https://doi.org/10.1016/0960-894X(95)00020-T
State	Published - Feb 2 1995

Bibliographical note

Funding Information:
Financial support from the National Institutes of Health (CA 55141 and CA55100) is acknowledged. The Danish Research Academy ($930093) and Familien Hede Nielsens Fond are acknowledged for grants to Lise Falborg. Support is also acknowledged from the Scientific Education Partnership of Marion Merr¢ll Dow for a postdoctoral fellowship awarded to Thomas C. Boge and from the Kansas Health Foundation for a postdoctoral fellowship awarded to Syed M. AlL We arc grateful for the excellent technical assistance of Ms. Christine

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title = "Synthesis of biologically active 2-benzoyl paclitaxel analogues",

abstract = "The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma cells. Most of the analogues were found to possess biological properties similar to paclitaxel.",

author = "Georg, {Gunda I.} and Ali, {Syed M.} and Boge, {Thomas C.} and Apurba Datta and Lise Falborg and Haeil Park and Marisan Mejillano and Himes, {Richard H.}",

note = "Funding Information: Financial support from the National Institutes of Health (CA 55141 and CA55100) is acknowledged. The Danish Research Academy ($930093) and Familien Hede Nielsens Fond are acknowledged for grants to Lise Falborg. Support is also acknowledged from the Scientific Education Partnership of Marion Merr¢ll Dow for a postdoctoral fellowship awarded to Thomas C. Boge and from the Kansas Health Foundation for a postdoctoral fellowship awarded to Syed M. AlL We arc grateful for the excellent technical assistance of Ms. Christine",

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doi = "10.1016/0960-894X(95)00020-T",

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T1 - Synthesis of biologically active 2-benzoyl paclitaxel analogues

AU - Georg, Gunda I.

AU - Ali, Syed M.

AU - Boge, Thomas C.

AU - Datta, Apurba

AU - Falborg, Lise

AU - Park, Haeil

AU - Mejillano, Marisan

AU - Himes, Richard H.

N1 - Funding Information: Financial support from the National Institutes of Health (CA 55141 and CA55100) is acknowledged. The Danish Research Academy ($930093) and Familien Hede Nielsens Fond are acknowledged for grants to Lise Falborg. Support is also acknowledged from the Scientific Education Partnership of Marion Merr¢ll Dow for a postdoctoral fellowship awarded to Thomas C. Boge and from the Kansas Health Foundation for a postdoctoral fellowship awarded to Syed M. AlL We arc grateful for the excellent technical assistance of Ms. Christine

PY - 1995/2/2

Y1 - 1995/2/2

N2 - The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma cells. Most of the analogues were found to possess biological properties similar to paclitaxel.

AB - The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma cells. Most of the analogues were found to possess biological properties similar to paclitaxel.

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Synthesis of biologically active 2-benzoyl paclitaxel analogues

Abstract

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