Abstract:
:2-Acetyl-(6-picolyl)-4N-substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells. Numerous derivatives were as active against solid tumor growth as clinically useful agents. The agents inhibited L1210 DNA and RNA syntheses with inhibition of key regulatory enzyme activities of the purine pathway as well as nucleoside kinase activities. d[NTP] pools were reduced and DNA strand scission occurred. These agents were DNA topoisomerase II inhibitors with lower IC50 values than that of VP-16. However, they did not cause L1210 DNA protein linked breaks and actually protected against those breaks afforded by VP-16. The agents were not synergistic with VP-16 in reducing cell growth or DNA synthesis although they did reduce growth of L1210 cells in agar suspended media.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Miller MC 3rd,Bastow KF,Stineman CN,Vance JR,Song SC,West DX,Hall IHdoi
10.1002/(sici)1521-4184(199804)331:4<121::aid-ardpsubject
Has Abstractpub_date
1998-04-01 00:00:00pages
121-7issue
4eissn
0365-6233issn
1521-4184pii
10.1002/(SICI)1521-4184(199804)331:4<121::AID-ARDPjournal_volume
331pub_type
杂志文章abstract::A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell ...
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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doi:10.1002/ardp.19933260609
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更新日期:1999-05-01 00:00:00
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journal_title:Archiv der Pharmazie
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pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:1999-11-01 00:00:00