当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Synthesis, molecular docking and cytotoxicity evaluation of novel 2-(4-amino-benzosulfonyl)-5H-benzo[b]carbazole-6,11-dione derivatives as histone deacetylase (HDAC8) inhibitors.

Synthesis, molecular docking and cytotoxicity evaluation of novel 2-(4-amino-benzosulfonyl)-5H-benzo[b]carbazole-6,11-dione derivatives as histone deacetylase (HDAC8) inhibitors.

Abstract：

:A new series of 2-(4-aminobenzosulfonyl)-5H-benzo[b]carbazole-6,11-dione derivatives, which has not been reported yet, has been synthesized from 1,4-naphthoquinone and 4-aminophenylsulfone involving an Michael addition, benzoylation and Pd catalyzed coupling. This set of compounds has been evaluated for in vitro cytotoxicity specifically against human cervical cancer cell line (SiHa) and most of the synthesized compounds exhibited good cytotoxic activity. Molecular docking of all the synthesized compounds was studied; among fourteen molecules docked compound 3 was the one with the best glide and E model score of -9.06 and -73.41, respectively which is close to the glide score of SAHA (standard). In all docked molecules, the compound 7a exhibits least glide and E model score of -2.97 and -71.02 respectively.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Ravichandiran P,Jegan A,Premnath D,Periasamy VS,Muthusubramanian S,Vasanthkumar S

doi

10.1016/j.bioorg.2014.01.002

subject

Has Abstract

pub_date

2014-04-01 00:00:00

pages

24-36

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(14)00006-6

journal_volume

53

pub_type

杂志文章

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