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Molecular Pharmacology

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Abstract

Structure-function studies with derivatives of 6-benzyl-1,3-benzodioxole, a new class of synthetic compounds which inhibit tubulin polymerization and mitosis.

J K Batra, L Jurd and E Hamel
Molecular Pharmacology January 1985, 27 (1) 94-102;
J K Batra
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L Jurd
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E Hamel
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Abstract

A new class of synthetic antineoplastic compounds, derivatives of 6-benzyl-1,3-benzodioxole, has significant antimitotic activity. These compounds inhibit microtubule assembly and are competitive inhibitors of the binding of colchicine to tubulin. Both their structure and their partial inhibition of tubulin-dependent GTP hydrolysis indicate that they are most comparable to podophyllotoxin of all known antimitotic drugs. Maximum activity required an intact dioxole ring, a methoxy or ethoxy substituent at position 5, and, on the benzyl moiety at position 6, a para-methoxy group. Additional methoxy groups on the benzyl substituent, to increase the apparent structural similarity to podophyllotoxin, resulted in major reduction of the antitubulin activity of these drugs.

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Molecular Pharmacology
Vol. 27, Issue 1
1 Jan 1985
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Abstract

Structure-function studies with derivatives of 6-benzyl-1,3-benzodioxole, a new class of synthetic compounds which inhibit tubulin polymerization and mitosis.

J K Batra, L Jurd and E Hamel
Molecular Pharmacology January 1, 1985, 27 (1) 94-102;

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Abstract

Structure-function studies with derivatives of 6-benzyl-1,3-benzodioxole, a new class of synthetic compounds which inhibit tubulin polymerization and mitosis.

J K Batra, L Jurd and E Hamel
Molecular Pharmacology January 1, 1985, 27 (1) 94-102;
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