Design, Synthesis, and Anticancer Properties of Novel Benzophenone‐Conjugated Coumarin Analogs

Abstract

In the current scenario, development of anticancer drugs with specific targets is of prime importance in modern chemical biology. Observing the importance of benzophenone and coumarin nucleus, it would be worthwhile to design and synthesize novel benzophenone derivatives (8a-o) bearing the coumarin nucleus. Further, they were screened for prospective anticancer activities in vitro against the Michigan Cancer Foundation-7 (MCF-7) and Ehrlich's ascites tumor (EAT) cell lines and their biomarkers, followed by in silico studies regarding phosphoinositide 3-kinase (PI3K) and caspase by molecular docking. Benzophenones have been reported as potential drugs targeting tumor angiogenesis; thus, the formation of neovessels in an in vivo model system like CAM, which is angiogenesis dependent, was observed in the presence of compounds 8a-o. The above findings would help in understanding their putative potential as therapeutic agents for cancer patients.

Evaluating the inhibitory potential ofWithania somniferaon platelet aggregation and inflammation enzymes: Anin vitroandin silicostudy

“…Docking studies revealed that withaferin A has higher potency of affinity than the standard drugs on the inflammatory enzymes COX-1, sPLA 2 and 5-LOX ( Figure 2) and which is evident through their hydrogen bonding with atomic contact energy (ACE) values as indicated (Table 1) 382, Arg 395, Tyr 396 and Tyr 614 with an atomic contact energy value of À128.96 as compared with standard phenidone (À103.61). Similar studies on bioactives have been mainly studies for retro synthesis mechanism (Begum et al 2013;Lakshmi Ranganatha et al 2013). Hence, the current study may thus emphasise the role of withaferin A as they offer better contribution in understanding the inflammatory enzyme activities besides their stability under physiological conditions.…”

“…There is no single docking algorithm or scoring function that can correctly predict the binding affinities of ligand in molecular interaction. For these reasons, in the present study, a highly validated docking program such as the ligand fit method in molegro package (Molegro ApS, Aarhus, Denmark) was used to investigate and identify the interaction of ligand molecule in the active region of the protein and to predict the binding affinity between the ligand and the receptor protein molecule using atomic contact energy (ACE) values (Lakshmi Ranganatha et al 2013).…”

Facile Synthesis and Anticancer Activity Study of Novel Series of Substituted and Fused Coumarin Derivatives

“…Literature survey revealed the significant anticancer activity of different coumarin derivatives against various cancer cell lines including HepG2 and MCF7 cell lines [10][11][12][13][14][15][16][17][18]. Therefore, Novel pyranocoumarin-4-carboxylate derivative 2 was prepared by fusion of the 5-hydroxycoumarin derivative 1 [19] and dimethyl acetylenedicarboxylate (Scheme 1).…”

“…Dark brown powder; yield: 0.1 g (31%); m. 6,6 ‚ -((4-Methoxyphenyl)methylene)bis(5-hydroxy-4,7-dimethyl-2H-chromen-2-one) (13). Dark brown powder; yield: 0.1 g (31%); m. 6,6 ‚ -((4-Methoxyphenyl)methylene)bis(5-hydroxy-4,7-dimethyl-2H-chromen-2-one) (13).…”

Synthesis and Characterization of Coumarin Analogs: Evaluation of Antimicrobial and Antioxidant Activities

“…In particular, coumarins and their derivatives have acquired much attention from the pharmacological and pharmaceutical arena due to their broad range of therapeutic qualities [4][5][6] . Numerous coumarin analogs have been reported as potential antibacterial 7 , antifungal 8 , antiinflammatory 9 , antioxidants 10 , anticancer and anti-HIV 11 agents.…”