Design and Synthesis of C3-Pyrazole/Chalcone-Linked Beta-Carboline Hybrids: Antitopoisomerase I, DNA-Interactive, and Apoptosis-Inducing Anticancer Agents

A series of β‐carboline hybrids bearing a substituted phenyl and a chalcone/(N‐acetyl)‐pyrazole moiety at the C1 and C3 positions, respectively, was designed, synthesized, and evaluated for anticancer activity. These new hybrid molecules showed significant cytotoxic activity, with IC50 values rangin...

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Published in:ChemMedChem 2014-09, Vol.9 (9), p.2084-2098
Main Authors: Kamal, Ahmed, Srinivasulu, Vunnam, Nayak, V. Lakshma, Sathish, Manda, Shankaraiah, Nagula, Bagul, Chandrakant, Reddy, N. V. Subba, Rangaraj, Nandini, Nagesh, Narayana
Format: Article
Language:English
Subjects:
anticancer activity
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
beta-carboline hybrids
Carbolines - chemical synthesis
Cell Cycle - drug effects
Cell Line, Tumor
Chalcones - chemistry
DNA binding
DNA Cleavage - drug effects
DNA photocleavage
DNA, Neoplasm - drug effects
Drug Screening Assays, Antitumor
Humans
Models, Molecular
Pyrazoles - chemistry
Topoisomerase I Inhibitors - chemical synthesis
Topoisomerase I Inhibitors - pharmacology
topoisomerase I inhibition
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Summary:A series of β‐carboline hybrids bearing a substituted phenyl and a chalcone/(N‐acetyl)‐pyrazole moiety at the C1 and C3 positions, respectively, was designed, synthesized, and evaluated for anticancer activity. These new hybrid molecules showed significant cytotoxic activity, with IC50 values ranging from
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201300406