Halohydrin analogues of cryptophycin 1: Synthesis and biological activity

Gunda I. Georg; Syed M. Ali; Valentine J. Stella; Wanda N. Waugh; Richard H. Himes

doi:10.1016/S0960-894X(98)00356-4

Halohydrin analogues of cryptophycin 1: Synthesis and biological activity

Gunda I. Georg, Syed M. Ali, Valentine J. Stella, Wanda N. Waugh, Richard H. Himes

Medicinal Chemistry

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Abstract

The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biological activities of the compounds were tested in an in vitro microtubule assembly and a cell proliferation assay. The chloro-derivative 2 showed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay.

Original language	English (US)
Pages (from-to)	1959-1962
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	15
DOIs	https://doi.org/10.1016/S0960-894X(98)00356-4
State	Published - Aug 4 1998

Bibliographical note

Funding Information:
Acknowledgments. These studies were supported by NIH research grant CA70369. S. M. Ali was a recipient of a postdoctoral scholar grant from the Kansas Health Foundation. Cryptophycin 1 was kindly supplied by R. E. Schwartz, Merck, Sharp & Dohme Research Laboratories.

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title = "Halohydrin analogues of cryptophycin 1: Synthesis and biological activity",

abstract = "The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biological activities of the compounds were tested in an in vitro microtubule assembly and a cell proliferation assay. The chloro-derivative 2 showed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay.",

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note = "Funding Information: Acknowledgments. These studies were supported by NIH research grant CA70369. S. M. Ali was a recipient of a postdoctoral scholar grant from the Kansas Health Foundation. Cryptophycin 1 was kindly supplied by R. E. Schwartz, Merck, Sharp & Dohme Research Laboratories.",

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AU - Stella, Valentine J.

AU - Waugh, Wanda N.

AU - Himes, Richard H.

N1 - Funding Information: Acknowledgments. These studies were supported by NIH research grant CA70369. S. M. Ali was a recipient of a postdoctoral scholar grant from the Kansas Health Foundation. Cryptophycin 1 was kindly supplied by R. E. Schwartz, Merck, Sharp & Dohme Research Laboratories.

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AB - The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biological activities of the compounds were tested in an in vitro microtubule assembly and a cell proliferation assay. The chloro-derivative 2 showed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay.

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Halohydrin analogues of cryptophycin 1: Synthesis and biological activity

Abstract

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