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Full-Text Articles in Other Chemicals and Drugs
Novel 3,6-Disubstituted Pyridazine Derivatives Targeting Jnk1 Pathway: Scaffold Hopping And Hybridization-Based Design, Synthesis, Molecular Modeling, In Vitro And In Vivo Anticancer Evaluation., Mai M. Shaalan, Essam Eldin A. Osman, Yasmeen M. Attia, Olfat A. Hammam, Riham F. George, Bassem H. Naguib
Novel 3,6-Disubstituted Pyridazine Derivatives Targeting Jnk1 Pathway: Scaffold Hopping And Hybridization-Based Design, Synthesis, Molecular Modeling, In Vitro And In Vivo Anticancer Evaluation., Mai M. Shaalan, Essam Eldin A. Osman, Yasmeen M. Attia, Olfat A. Hammam, Riham F. George, Bassem H. Naguib
Pharmacy
A series of novel 3,6-disubstituted pyridazine derivatives was designed, synthesized, and biologically evaluated as preclinical anticancer candidates. Compound 9e exhibited the highest growth inhibition against most of the NCI-60 cancer cell lines. The in vivo anticancer activity of 9e was subsequently investigated at two dose levels using the Ehrlich ascites carcinoma solid tumor animal model where a reduction in the mean tumor volume allied with necrosis induction was reported, without any signs of toxicity in the treated groups. Interestingly, compound 9e was capable of downregulating c-jun N-terminal kinase-1 (JNK1) gene expression and curbing the protein levels of its phosphorylated form, …
Synthesis And Biological Evaluation Of New Nicotinic Acid Derivatives As Potential Anti-Inflammatory Agents With Enhanced Gastric Safety Profile, Eman Ramadan, Zeinab Mahmoud, Nadia Khalil
Synthesis And Biological Evaluation Of New Nicotinic Acid Derivatives As Potential Anti-Inflammatory Agents With Enhanced Gastric Safety Profile, Eman Ramadan, Zeinab Mahmoud, Nadia Khalil
Pharmacy
Two innovative series derived from nicotinic acid scaffold were synthesized and evaluated for their anti-inflammatory activity. Ibuprofen, celecoxib and indomethacin were used as standard drugs. All the newly synthesized compounds were in vitro screened for their anti-inflammatory activity adopting 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide dye (MTT), as well as Griess assays. The results showed that all compounds exhibited significant anti-inflammatory activity without affecting the viability of the macrophages compared to ibuprofen. In addition, compounds 4d, 4f, 4g, 4h and 5b exhibited the most potent nitrite inhibition activity and consequently superior anti-inflammatory activity with MTT results ranging between values 86.109 ± 0.51 to 119.084 …
Design, Synthesis, And Anti-Mcf-7 Activity Of New Thieno[2,3-D]Pyrimidinone Derivatives As Potential Breast Cancer Treatment, Bassem H. Naguib, Amgad Albohy, Mostafa A. Abdelaziz, Hanan H. Kadry
Design, Synthesis, And Anti-Mcf-7 Activity Of New Thieno[2,3-D]Pyrimidinone Derivatives As Potential Breast Cancer Treatment, Bassem H. Naguib, Amgad Albohy, Mostafa A. Abdelaziz, Hanan H. Kadry
Pharmacy
Breast cancer is one of the top leading causes of death and the most aggressive type of cancer in women. Resistance to chemotherapy is one of the challenges associated with the development of strategies for the treatment of breast cancer. One way to overcome this issue is to design new agents that target breast cancer cell lines such as MCF-7. In this study, a new series of S-alkylated thieno[2,3-d]pyrimidin-4-ones bearing carboxamide or ketonic scaffolds was synthesized and screened for their cytotoxicity against MCF-7 breast cell lines. Among synthesized candidates, 6d exhibited more potent cytotoxicity against MCF-7 cell lines with IC50 …
Development Of Rp-Hplc Method For Simultaneous Determination Of Nebivolol Hydrochloride, Valsartan And Hydrochlorothiazide In Co-Administrated Antihypertensive Agents And Human Plasma, Shereen Mowaka, M. Rizk, Maha M. Abou El‐Alamin, Mariam Mohamed
Development Of Rp-Hplc Method For Simultaneous Determination Of Nebivolol Hydrochloride, Valsartan And Hydrochlorothiazide In Co-Administrated Antihypertensive Agents And Human Plasma, Shereen Mowaka, M. Rizk, Maha M. Abou El‐Alamin, Mariam Mohamed
Pharmacy
Reversed phase high performance liquid chromatography combined with photodiode array (HPLC-PDA) detector method was developed for simultaneous determination of two binary antihypertensive combinations; either Nebivolol (NEB) with Hydrochlorothiazide (HCZ) or with Valsartan (VAL) in pharmaceutical formulation and spiked human plasma. The method was successfully applied to separate the three drugs on one chromatogram under the same chromatographic conditions that used for two binary combinations. The separation was established on Xterra C18 column using gradient mobile phase which composed of acidified water of pH = 3.0 (adjusted with 0.1% orthophosphoric acid) and acetonitrile with flow rate of 1.0 mL/min. The drugs …
Omarigliptin Attenuates Rotenone-Induced Parkinson's Disease In Rats: Possible Role Of Oxidative Stress, Endoplasmic Reticulum Stress And Immune Modulation, Shereen Mowaka, Haidy E. Michel, Mariam M. Tadros, Moataz S. Hendy, Bassam M. Ayoub
Omarigliptin Attenuates Rotenone-Induced Parkinson's Disease In Rats: Possible Role Of Oxidative Stress, Endoplasmic Reticulum Stress And Immune Modulation, Shereen Mowaka, Haidy E. Michel, Mariam M. Tadros, Moataz S. Hendy, Bassam M. Ayoub
Pharmacy
The current study aimed to explore the potential neuroprotective effect of omarigliptin (OG), an antidiabetic drug that crosses the blood-brain barrier (BBB), in a Parkinson's disease (PD) rotenone-based rat-model. Results showed that OG attenuated motor impairment, histological aberrations, α-synuclein accumulation, and rescued the dopaminergic neurons in rotenone-administered rats. Furthermore, OG halted rotenone-induced oxidative stress; as shown by reduced lipid peroxidation, decline in the oxidative stress sensor (nuclear factor erythroid 2-related factor 2) and its downstream heme oxygenase-1. In addition, OG abrogated neuroinflammation and apoptosis in rotenone-treated rats. Moreover, OG ameliorated endoplasmic reticulum (ER) stress in rotenone-administered rats; as evidenced by …