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Synthesis of methotrexate-antibody conjugates by regiospecific coupling and assessment of drug and antitumor activities.

Abstract：

:In order to increase the retention of drug activity, regiospecific coupling has been used to synthesize conjugates of methotrexate (MTX, 1) with normal rabbit IgG (NRG) and a mouse anti-human renal cancer monoclonal IgG (Dal K-20). MTX gamma-methyl ester (4) was produced either by selective esterification of MTX or by coupling of 4-amino-4-deoxy-N10-methylpteroic acid (2) with suitable glutamic acid derivatives. The MTX gamma-methyl ester (4) was then converted to the corresponding hydrazide 6. An amide-linked conjugate was formed when the MTX gamma-hydrazide (6) was converted to reactive acylating species 7 by using tert-butyl nitrite or trifluoroacetaldehyde, which were reacted with nucleophilic centers, presumably epsilon-amino groups, in native IgG. A hydrazone-linked conjugate was formed when MTX gamma-hydrazide (6) was reacted directly with IgG that had first been oxidized with periodate to form polyaldehyde IgG. The regiospecifically synthesized conjugates were somewhat more effective inhibitors in vitro of dihydrofolate reductase and of colony formation by human renal cancer (Caki-1) cells than were control nonregiospecific conjugates.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kralovec J,Spencer G,Blair AH,Mammen M,Singh M,Ghose T

doi

10.1021/jm00131a003

subject

Has Abstract

pub_date

1989-11-01 00:00:00

pages

2426-31

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

32

pub_type

杂志文章

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