116589-50-5Relevant academic research and scientific papers
Synthesis and biological evaluation of new coumarin derivatives as cytotoxic agents
Ragab, Fatma A.,Eissa, Amal A. M.,Fahim, Samar H.,Salem, Mohammad A.,Gamal, Mona A.,Nissan, Yassin M.
, (2021/05/03)
New coumarin derivatives 9a–f, 10a–e, and 11a–f were synthesized and evaluated for their cytotoxic activity against a human breast cancer cell line (MCF-7). All compounds exhibited good activity in the nanomolar range, using doxorubicin and erlotinib as positive controls. The most active compound 9d with IC50 of 21 nM was tested against the HCT-116, HepG-2, A549, and SGC-7901 cell lines, with IC50 values of 0.021, 0.170, 0.028, and 0.11 μM, respectively. Compound 9d was further investigated for its ability to suppress the expression of epidermal growth factor receptor (EGFR). Compound 9d decreased the concentration of EGFR by 87%, using erlotinib as a positive control. A docking study revealed similar or higher scores than for erlotinib and similar binding poses providing interactions with the hinge region of the tyrosine kinase (TK). Besides the effect on expression, this in silico investigation predicts the possibility of direct binding between the new coumarin derivatives and the EGFR TK. Moreover, computational calculation for ADME properties for the most active compounds 9d, 9e, 10c, and 11c revealed the expected high gastrointestinal tract absorption, moderate water solubility with no central nervous system toxicity, and druglikeness.
Synthesis of modified pyridine and bipyridine substituted coumarins as potent antimicrobial agents
Lad, Hemali B.,Giri, Rakesh R.,Chovatiya, Yogita L.,Brahmbhatt, Dinkar I.
, p. 739 - 747 (2015/08/24)
In the search for new antimicrobial agents, a series of new modified pyridine and bipyridine substituted coumarins 5a-y was designed and synthesized by adopting a molecular hybridization strategy. All the synthesized compounds were evaluated for their in
Microwave-assisted synthesis of 4-methyl-8-aryl-pyrano [2,3-f] chromen-2,10-diones and their antibacterial activity
Ashok,Vijaya Lakshmi,Ganesh, Arram,Ravi
, p. 331 - 334 (2019/01/21)
A series of 4-methyl-8-aryl-pyrano [2,3-f] chromen-2,10-diones have been synthesized by oxidative cyclization of 7-hydroxy-4-methyl-8-(3-aryl acrolyl)-2Hchromen- 2-ones using I2/DMSO under microwave irradiation. The structures of the synth
Solvent-free microwave assisted synthesis of 8-acetyl-4-methyl-9-styryl-2H- furo [2,3-h] chromen-2-ones and their antibacterial activity
Ashok,Vijaya Lakshmi
, p. 337 - 340 (2013/09/24)
A new series of 8-acetyl-4-methyl-9-styryl-2H-furo [2,3-ft] chromen-2-ones have been synthesized by cyclisation of 7-hydroxy-4-methyl-8-(3-aryl acrolyl)-2W-chromen-2-ones with chloroacetone. The structures of the synthesized compounds have been establishe
Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide
Rathish,Javed, Kalim,Ahmad, Shamim,Bano, Sameena,Alam,Pillai,Singh, Surender,Bagchi, Vivek
scheme or table, p. 255 - 258 (2009/05/07)
Nineteen new 2-pyrazoline bearing benzenesulfonamide derivatives were synthesized by condensing chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride. Their chemical structures were proved by means of IR, 1H NMR, 13C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of 20 mg/kg for their anti-inflammatory activity in carrageenan-induced rat paw edema model and volume of paw edema was measured at 0, 3 and 5 h. Two compounds 3k and 3l were found to be more active than celecoxib throughout the study (at 3 and 5 h). While two other compounds 3m and 3n showed more potent activity than celecoxib at 5 h. They are devoid of ulcerogenic potential when administered orally at a dose of 60 mg/kg. Compounds (3k-m) showed COX-1 and COX-2 inhibitory activity at 0.05 μM.
Synthesis and antiinflammatory activity of benzopyran-2-ones and their derivatives
Bhalla, Manish,Naithani, P K,Kumar, A,Bhalla, T N,Shanker, K
, p. 183 - 186 (2007/10/02)
Various substituted benzopyran-2-ones (2,4,5 and 7) have been synthesized from 8-acetyl-7-hydroxy-4-methyl-2H-1-benzopyran-2-one (1) by appropriate methods.The benzopyrans 2 and 5 have been converted into 1-acetyl-5-substituted phenyl/indol-3-yl-3-(7-hydr
