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5‐Substituted 2‐Bromoindolo[3,2‐ b ]quinoxalines. A Class of Potential Antitumor Agents with cdc25 Phosphatase Inhibitory Properties
Author(s) -
Abadi Ashraf H.
Publication year - 1998
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(199811)331:11<352::aid-ardp352>3.0.co;2-2
Subject(s) - cdc25 , phosphatase , chemistry , cyclin dependent kinase 1 , quinoxaline , kinase , ic50 , inhibitory postsynaptic potential , in vitro , stereochemistry , biochemistry , pharmacology , phosphorylation , biology , cell cycle , organic chemistry , apoptosis , endocrinology
Several derivatives of 5‐substituted‐2‐bromoindolo[3,2‐ b ]quinoxaline were synthesized and characterized. The synthesized compounds were evaluated for their antitumor activity using the National Cancer Institute‐ in vitro ‐disease oriented antitumor screen and two biochemical mechanism‐based screens (cdc2 kinase and cdc25 phosphatase). Compound 19 showed broad spectrum antitumor activity with full panel (MG‐MID) GI 50 , TGI, and LC 50 of 14.2, 31.6‐ and 66.2 μM, respectively. In addition it inhibited cdc2 kinase and cdc25 phosphatase with IC 50 ’s of 70 and 25 μM, respectively. Thus, compound 19 represents a model for compounds with potential antitumor activity and cdc25 phosphatase inhibitory properties.