687639-17-4Relevant academic research and scientific papers
Design, synthesis and pharmacological evaluation of 2-phenyl quinazolin-4-one derivatives as anticolorectal cancer and anti-inflammatory agent
Bosco, Deena,Balakrishnan, Ashitha,Mishra, Rohan,Aneesh
, p. 2677 - 2685 (2018/11/20)
Quinazoline derivatives are heterocyclic compounds that acts as important structural lead for the discovery of effective therapeutic agents. The anti-inflammatory activity along with cytotoxicity helps to reduce the inflammation and pain associated with carcinoma. Derivatives of quinazoline-4-one were preliminary screened and in silico molecular modelling studies using Autodock were performed. In the docking study, ligands were docked against anticancer and anti-inflammatory targets. In silico analysis revealed that the compounds with aromatic substitution at 3rd and halogen substitution at 6th or 7th positions possess lesser side effects and have more potent antitumor activity. Based upon these results 12 compounds were selected, synthesized, characterized and screened for their in vitro, anti-inflammatory, antioxidant and anticancer activities. From the in vitro studies, compounds QA4, QA7 and QB1 showed good anticancer, anti-inflammatory and antioxidant activity when compared to the standard.
Synthesis and evaluation of fused pyrimidine derivatives as anti-inflammatory, antiproliferative and antimicrobial agents
Vachala, Seekarajapuram Dinakaran,Srinivasan, Keloth Kothari,Prakash, Peralam Yegneswaran
, p. 2998 - 3005 (2012/10/30)
In this study, condensation of 2-amino-5-chlorobenzoic acid with benzoyl chloride afforded 2-benzamido-5- chloro benzoic acid which on cyclization with different primary amines yielded the corresponding 6-chloro-2-phenyl- 3-substituted quinazolin-4(3H)-ones (V1-V8). The reaction was monitored by thin layer chromatographic analysis. The structure of the synthesized compounds was confirmed by spectral studies and elemental analysis. All these compounds were screened for their anti-inflammatory, antiproliferative and antimicrobial activities. Anti-inflammatory activity was done by rat paw oedema method. Compounds V6 and V5 showed a good percentage inhibition of inflammation at the 2nd and the 3rd h, respectively. Antiproliferative activity was carried out byMTT assay againstChang liver,Hep2 andHeLa cell lines. Compounds V1, V5 and V8 showed antiproliferative activity at low concentrations. The minimum inhibitory concentrations (MIC) of the synthesized compounds against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Candida albicans and Aspergillus flavus was studied by microdilution assay. Compound V4 was found to be a potent antimicrobial agent against the organisms tested. Further, itwas selected for time kill study. These data revealed that the compounds containing chloro- and/or fluoro-substituted phenyl ring or N,N-dimethyl ethyl substitutions in the quinazolin-4(3H)-ones led to increase of their biological activities. Springer Science+Business Media, LLC 2011.
