Synthesis and in vitro anticancer and antitubercular activity of diarylpyrazole ligated dihydropyrimidines possessing lipophilic carbamoyl group

A series of dihydropyrimidine derivatives were synthesized by utilizing Biginelli reaction and evaluated for their in vitro anticancer activity against MCF-7 human breast cancer (HBC) cell line using sulforhodamine B (SRB) assay and antitubercular activity against Mycobacterium tuberculosis (MTB) H3...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-04, Vol.22 (8), p.2708-2711
Main Authors: Yadlapalli, Rama Krishna, Chourasia, O.P., Vemuri, Kiranmayi, Sritharan, Manjula, Perali, Ramu Sridhar
Format: Article
Language:English
Subjects:
1,3-Diarylpyrazoles
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Anticancer
anticarcinogenic activity
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Antitubercular
Antitubercular Agents - chemical synthesis
Antitubercular Agents - pharmacology
Antitumor activity
Biological and medical sciences
Breast cancer
breast neoplasms
Breast Neoplasms - drug therapy
Carbamates - chemistry
cell growth
Cell Line, Tumor
Cell Proliferation - drug effects
Dihydropyrimidines
Dose-Response Relationship, Drug
Female
General aspects
Humans
Lipids - chemistry
Lipophilic
Medical sciences
Microbial Sensitivity Tests
Minimum inhibitory concentration
Molecular Structure
Multicomponent Reaction
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Solubility
sulforhodamine
Tumor cell lines
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Summary:A series of dihydropyrimidine derivatives were synthesized by utilizing Biginelli reaction and evaluated for their in vitro anticancer activity against MCF-7 human breast cancer (HBC) cell line using sulforhodamine B (SRB) assay and antitubercular activity against Mycobacterium tuberculosis (MTB) H37Rv using Microplate Alamar Blue Assay (MABA). Compounds 13p, 13t were exhibited 70.6% and 63.7% of HBC cell growth inhibition at 10μM concentration. Interestingly compound 13p was also found to be the most potent in the series against MTB H37Rv with MIC value of 0.125μg/mL.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.02.101