925408-64-6Relevant academic research and scientific papers
Quinoxaline-PABA bipartite hybrid derivatization approach: Design and search for antimicrobial agents
Patel, Harun M.,Bhardwaj, Varun,Sharma, Poonam,Noolvi, Malleshappa N.,Lohan, Sandeep,Bansal, Sumit,Sharma, Amit
, p. 562 - 568 (2019)
In an attempt to find a new class of antimicrobial agents, in the present study we report the synthesis of bipartite hybrid styryl derivatives of quinoxaline containing para-aminobenzoic acid (PABA) and their biological evaluation as antimicrobial agents. The series of new substituted styryl based derivatives 5(a–k) were evaluated for antimicrobial potential against various bacteria including Staphylococcus aureus, Vibrio cholerae, Escherichia coli, Bacillus subtilis, Escherichia coli, Mycobacterium smegmatis, Pseudomonas aeruginosa and fungi; C. albicans, with ampicillin and amphotericin B as standards. Similarly these compounds were also screened for anti-cancer activity using MCF-7 cell line. Among the synthesized compounds, 5(c) was observed to be the most active compound against various strains with MIC in a range of 7.9–31 μM of the series and compound 5i came out with significant anti-cancer activity with IC50 value of 7 μM.
Synthesis and in vitro antitumor activity of substituted quinazoline and quinoxaline derivatives: Search for anticancer agent
Noolvi, Malleshappa N.,Patel, Harun M.,Bhardwaj, Varun,Chauhan, Ankit
, p. 2327 - 2346 (2011/06/25)
The synthesis of some 2-furano-4(3H)-quinazolinones, diamides (open ring quinazolines), quinoxalines and their biological evaluation as antitumor agents using National Cancer Institute (NCI) disease oriented antitumor screen protocol are investigated. Among the synthesize compounds, seventeen compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the selected compounds, 3-(2-chloro benzylideneamine)-2- (furan-2-yl) quinazoline-4(3h)-one 21 was found to be the most active candidate of the series at five dose level screening against Ovarian OVCAR-4 and Non-small cell lung cancer NCI-H522 with GI50 1.82 & 2.14 μM respectively. Rational approach and QSAR techniques enabled the understanding of the pharmacophoric requirement for quinazoline, diamides and quinoxaline derivatives.
