89019-07-8Relevant articles and documents
5-Phenylcoumarin Derivatives: Design, Synthesis, and Vasodilatory Activity
Wang, Cheng,Li, Youjia,Zhang, Ting,Wei, Di,Hou, Yajing,He, Huaizhen
, (2018/11/01)
In continuation of our previous efforts towards the development of coumarin derivatives with potential vasodilatory activity, 5-phenylcoumarin derivatives were designed and synthesized. Target compounds and their precursors exhibited moderately vasodilato
Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells
Amin, Kamilia M.,Abou-Seri, Sahar M.,Awadallah, Fadi M.,Eissa, Amal A.M.,Hassan, Ghaneya S.,Abdulla, Mohamed M.
, p. 221 - 231 (2015/05/04)
Based on the reported anticancer activity of coumarin and pyrazoline derivatives, the present investigation dealt with the design and synthesis of coumarin derivatives bearing diversely substituted pyrazoline moieties 7-10. The non-cyclic isosteres 11a-e
Design, synthesis and vasorelaxant evaluation of novel coumarin-pyrimidine hybrids
Amin, Kamilia M.,Awadalla, Fadi M.,Eissa, Amal A.M.,Abou-Seri, Sahar M.,Hassan, Ghaneya S.
scheme or table, p. 6087 - 6097 (2011/11/06)
The main objective of the present work depends on the hybridization of coumarin moiety as a vasorelaxant scaffold and pyrimidine ring with known potential cardiovascular activity in order to prepare some new potent antihypertensive candidates. Hence, two groups of pyrimidinyl coumarin derivatives were synthesized and evaluated for their vasorelaxing activity. These compounds were prepared via two routes; either preparation of the guanidinocoumarin 4 followed by a cocktail of cyclization reactions to yield a different array of 6-(substituted pyrimidin-2-yl)aminocoumarins 5-17, or through cyclization of the precursor chalcones 22a-g with guanidine hydrochloride to generate the corresponding final compounds, 8-(6-aryl-2-aminopyrimidin-4-yl)-7- methoxycoumarins 23a-g. The effect of these compounds and the coumarin intermediates 3, 4, 21 and 22a-g on nor-epinephrine induced contracture in thoracic rat aortic rings was investigated using prazocin as reference drug. Several derivatives showed promising activities either equal or even better than that of prazocin (IC50 0.487 mM). The most prospective compounds; the pyrimidinylamino coumarin derivatives 8, 17 (IC50 0.411, IC 50 0.421 mM) and the chalcones 22b, 22e (IC50 0.371, 0.374 mM) that displayed the highest activity can be a base for lead optimization and simple but efficient design of new compounds. 2D-QSAR analysis was applied to find a correlation between the experimental vasorelaxant activities of the newly synthesized coumarin derivatives and their different physicochemical parameters. The result of this study showed that the increase in aqueous solubility while retaining good hydrophobic character of the overall molecule is the key for maintaining high relaxation activity.
