Abstract：
:Newly synthesized benzamide derivatives were evaluated for their inhibitory activity against histone deacetylase. The structure of these derivatives was unrelated to the known inhibitors, and IC(50) values of the active compounds were in the range of 2-50 microM. Structure-activity relationship on the benzanilide moiety showed that the 2'-substituent, an amino or hydroxy group, was indispensable for inhibitory activity. Although the electronic influence of the substituent in the anilide moiety showed only a small effect on inhibitory activity, the steric factor in the anilide moiety, especially at positions 3'and 4', played an important role in interaction with the enzyme. Among these benzamide derivatives, MS-275 (1), which showed significant antitumor activity in vivo, has been selected for further investigation.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Suzuki T,Ando T,Tsuchiya K,Fukazawa N,Saito A,Mariko Y,Yamashita T,Nakanishi Odoi
10.1021/jm980565ukeywords:
subject
Has Abstractpub_date
1999-07-29 00:00:00pages
3001-3issue
15eissn
0022-2623issn
1520-4804pii
jm980565ujournal_volume
42pub_type
杂志文章abstract：:Oral PI3Kδ inhibitors such as Idelalisib and Duvelisib have shown efficacy as anticancer agents and Idelalisib has been approved for the treatment of three B-cell cancers. However, Idelalisib has a black box warning on its product label regarding the risks of fatal and serious toxicities including hepatic toxicity, se...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
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pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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pub_type： 杂志文章
doi：10.1021/jm00200a017
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journal_title：Journal of medicinal chemistry
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journal_title：Journal of medicinal chemistry
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doi：10.1021/jm00028a005
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00155a040
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm900576g
更新日期：2009-12-10 00:00:00
abstract：:A series of substituted benzenedisulfonamide carbonic anhydrase inhibitors is described and their anticonvulsant activities are listed. One compound, 4-(4-methoxypiperidinosulfonyl)-2-chlorobenzenesulfonamide (19, UK-12130), was found to have anticonvulsant activity in animals at a dose level that gave only a minimal ...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00207a001
更新日期：1978-09-01 00:00:00
