1421758-37-3Relevant academic research and scientific papers
Mechanism of antiangiogenic and antioxidant activity of newly synthesized CAMBA in ehrlich ascites carcinoma-bearing mice
Abou-Taleb, Nada I.,Ahmed, Fakher M.,Ali, Ali A.,Basuny, Haidy I.,Elbesoumy, Esraa A.,Elblasy, Ola A.,Elhamadi, Esraa A.,Emara, Ahmed A.,Hussein, Mohammed A.,Nasr Eldin, Mohamed S.,Salem, Mohamed A.
, p. 2465 - 2471 (2021/09/28)
The aim of present study was to evaluate antiangiogenic activity of newly synthesized caffeic acid methyl benzoate amide (CAMBA) in EAC-bearing mice. The IC50 value of CAMBA against the Hep-G2 liver carcinoma cell line was calculated. Adult albino mice weighing 25 ± 5 g was used to assess the antiangiogenic activity of CAMBA (25 and 50 mg/k.b.w.) in EAC-bearing mice. IC50 CAMBA against the Hep-G2 cell line equals 52.8 μg/mL. The daily oral administration of CAMBA at concentrations of 25 and 50 mg/kg.b.w. for 30 days to EAC-bearing mice resulted in a significant improvement in tumor volume and tumor weight, ALT, AST, ALP, MMP-2 and -9, TNF-α, NOx, TBARs, GSH, CAT, SOD, GPx and VEGF-C gene expression in EAC-bearing mice. Furthermore, CAMBA almost normalized these effects in liver histoarchitecture. The biochemical, histological and ultrasound examinations of our study suggested that CAMBA have antiangiogenic activity in EAC-bearing mice.
Design, synthesis, and evaluation of caffeic acid amides as synergists to sensitize fluconazole-resistant Candida albicans to fluconazole
Dai, Li,Zang, Chengxu,Tian, Shujuan,Liu, Wei,Tan, Shanlun,Cai, Zhan,Ni, Tingjunhong,An, Maomao,Li, Ran,Gao, Yue,Zhang, Dazhi,Jiang, Yuanying
, p. 34 - 37 (2015/02/19)
A series of caffeic acid amides were designed, synthesized, and their synergistic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The title caffeic acid amides 3-30 except 26 exhibited potent activity, and the subsequent SAR study was conducted. Compound 3, 5, 21, and 34c, at a concentration of 1.0 μg/ml, decreased the MIC80 of fluconazole from 128.0 μg/ml to 1.0-0.5 μg/ml against the fluconazole-resistant C. albicans. This result suggests that the caffeic acid amides, as synergists, can sensitize drug-resistant fungi to fluconazole. The SAR study indicated that the dihydroxyl groups and the amido groups linking to phenyl or heterocyclic rings are the important pharmacophores of the caffeic acid amides.
Synthesis, anti-inflammatory, and structure antioxidant activity relationship of novel 4-quinazoline
Hussein, Mohammed Abdalla
, p. 4641 - 4653 (2013/09/23)
The practice of medicinal chemistry is devoted to the discovery and development of new agents for treating disease. A new derivative of methyl 2-((E)-3-(3,4-dihydroxyphenyl)acrylamido)benzoate 2 was synthesized by reacting the amino group of methyl anthranilate 1 with caffeic acid in the presence of PCl3. Cyclcondensation of 2 with hydrazine hydrate afforded the corresponding 2,3-dihydro-2-(3,4-dihydroxyphenyl) pyrazolo[5,1-b]quinazolin- 9(1H)-one 3. The median lethal doses (LD50s) of compounds 2 and 3 in mice were 1,135 and 495 mg/kg b.w., respectively. The anti-inflammatory, reducing power, chelating activity on Fe2+, free radical-scavenging, and total antioxidant activities were more pronounced in compound 2 compared to compound 3. On the other hand, antipyretic activity was more pronounced in compound 3 compared to compound 2. Antioxidant activity of compounds 2 and 3 increased with increased concentrations. Total antioxidant activity of compounds 2, 3 and both standards decreased in the order of α-tocopherol > compound 2 > trolox > BHA > BHT > compound 3. Administration of compounds 2 and 3 orally to the rats at dose of 50, 100, and 150 mg/kg b.w., for 10 days showed non-significant changes in serum level of GOT, GPT, ALP, γ-GT, and LDH as compared with the control group. In addition, oral administration of the compound 2 at a concentration of 100 and 150 mg/kg b.w. and compound 3 at a concentration of 150 mg/kg b.w. daily to normal rats for 10 days showed a significant increase in liver GSH, GPx, GR, and GST activities and significant decrease in TBARS level. But, administration of diclofenac sodium (30 mg/kg b.w.) orally to the rats daily for 10 days to rats showed significant increase in serum SGOT, SGPT, ALP, γ-GT, and LDH and significant decrease in liver GSH, GPx, GR, and GST activities. These findings suggest that compounds 2 and 3 exhibited good antioxidant and anti-inflammatory activity and also showed effects on liver enzymes.
