scholarly journals Ginsenosides as anticancer agents: In vitro and in vivo activities, structure–activity relationships, and molecular mechanisms of action

2012 ◽  
Vol 3 ◽  
Author(s):  
Subhasree Ashok Nag
Keyword(s):  
Anticancer Agents ◽  
Molecular Mechanisms ◽  
Mechanisms Of Action ◽  
Structure Activity Relationships ◽  
Structure Activity

1,3,5-Triazine-azole Hybrids and their Anticancer Activity

2020 ◽  
Vol 20 (16) ◽  
pp. 1481-1492
Author(s):  
Hua Guo ◽  
Quan-Ping Diao
Keyword(s):  
Clinical Trials ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Mechanisms Of Action ◽  
Structure Activity ◽  
Hybrid Molecules ◽  
Excellent Activity ◽  
Enhance Efficiency

1,3,5-Triazine and azole can interact with various therapeutic targets, and their derivatives possess promising in vitro and in vivo anticancer activity. Hybrid molecules have the potential to enhance efficiency, overcome drug resistance and reduce side effects, and many hybrid molecules are under different phases of clinical trials, so hybridization of 1,3,5-triazine with azole may provide valuable therapeutic intervention for the treatment of cancer. Substantial efforts have been made to develop azole-containing 1,3,5-triazine hybrids as novel anticancer agents, and some of them exhibited excellent activity. This review emphasizes azole-containing 1,3,5-triazine hybrids with potential anticancer activity, and the structure-activity relationships as well as the mechanisms of action are also discussed to provide comprehensive and target-oriented information for the development of this kind of anticancer drugs.

Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents

2020 ◽  
Vol 44 (6) ◽  
pp. 2247-2255
Author(s):  
Qifan Zhou ◽  
Lina Jia ◽  
Fangyu Du ◽  
Xiaoyu Dong ◽  
Wanyu Sun ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Activity Assay ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Enhancer Of Zeste

A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with in vitro biological activity assay and docking results.

In Vivo and in Vitro Structure-Activity Relationships and Structural Conformation of Kisspeptin-10-Related Peptides

2009 ◽  
Vol 76 (1) ◽  
pp. 58-67 ◽  
Author(s):  
Ester Gutiérrez-Pascual ◽  
Jérôme Leprince ◽  
Antonio J. Martínez-Fuentes ◽  
Isabelle Ségalas-Milazzo ◽  
Rafael Pineda ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structural Conformation ◽  
Structure Activity

scholarly journals Structure-Activity Relationships of a Series of Echinocandins and the Discovery of CD101, a Highly Stable and Soluble Echinocandin with Distinctive Pharmacokinetic Properties

2016 ◽  
Vol 61 (2) ◽  
Author(s):  
Kenneth D. James ◽  
Christopher P. Laudeman ◽  
Navdeep B. Malkar ◽  
Radha Krishnan ◽  
Karen Polowy
Keyword(s):  
Pharmacokinetic Studies ◽  
Pharmacokinetic Data ◽  
Activity Data ◽  
Content Type ◽  
Structure Activity Relationships ◽  
First Line Therapy ◽  
Structure Activity ◽  
Pharmacokinetic Properties

ABSTRACT Echinocandins are a first-line therapy for candidemia and invasive candidiasis. They are generally safe with few drug interactions, but the stability and pharmacokinetic properties of currently approved echinocandins are such that each was developed for daily intravenous infusion. We sought to discover a novel echinocandin with properties that would enable more flexible dosing regimens, alternate routes of delivery, and expanded utility. Derivatives of known echinocandin scaffolds were generated, and an iterative process of design and screening led to the discovery of CD101, a novel echinocandin that has since demonstrated improved chemical stability and pharmacokinetics. Here, we report the structure-activity relationships (including preclinical efficacy and pharmacokinetic data) for the series of echinocandin analogs from which CD101 was selected. In a mouse model of disseminated candidiasis, the test compounds displayed clear dose responses and were generally associated with lower fungal burdens than that of anidulafungin. Single-dose pharmacokinetic studies in beagle dogs revealed a wide disparity in the half-lives and volumes of distribution, with one compound (now known as CD101) displaying a half-life that is nearly 5-fold longer than that of anidulafungin (53.1 h versus 11.6 h, respectively). In vitro activity data against panels of Candida spp. and Aspergillus spp. demonstrated that CD101 behaved similarly to approved echinocandins in terms of potency and spectrum of activity, suggesting that the improved efficacy observed in vivo for CD101 is a result of features beyond the antifungal potency inherent to the molecule. Factors that potentially contribute to the improved in vivo efficacy of CD101 are discussed.

scholarly journals Inhibitory effects of Lang-du extract on the in vitro and in vivo growth of melanoma cells and its molecular mechanisms of action

2010 ◽  
Vol 62 (4) ◽  
pp. 357-366 ◽  
Author(s):  
Liping Wang ◽  
Huiying Duan ◽  
Yishan Wang ◽  
Kun Liu ◽  
Peng Jiang ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Melanoma Cells ◽  
Mechanisms Of Action ◽  
Inhibitory Effects ◽  
In Vivo Growth

scholarly journals Structure-Activity Relationships of Bacillus cereus and Bacillus anthracis Dihydrofolate Reductase: toward the Identification of New Potent Drug Leads

2006 ◽  
Vol 50 (10) ◽  
pp. 3435-3443 ◽  
Author(s):  
Tammy M. Joska ◽  
Amy C. Anderson
Keyword(s):  
Bacillus Cereus ◽  
Bacillus Anthracis ◽  
Dihydrofolate Reductase ◽  
Antimicrobial Agents ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Phenyl Rings ◽  
Potent Drug

ABSTRACT New and improved therapeutics are needed for Bacillus anthracis, the etiological agent of anthrax. To date, antimicrobial agents have not been developed against the well-validated target dihydrofolate reductase (DHFR). In order to address whether DHFR inhibitors could have potential use as clinical agents against Bacillus, 27 compounds were screened against this enzyme from Bacillus cereus, which is identical to the enzyme from B. anthracis at the active site. Several 2,4-diamino-5-deazapteridine compounds exhibit submicromolar 50% inhibitory concentrations (IC50s). Four of the inhibitors displaying potency in vitro were tested in vivo and showed a marked growth inhibition of B. cereus; the most potent of these has MIC50 and minimum bactericidal concentrations at which 50% are killed of 1.6 μg/ml and 0.09 μg/ml, respectively. In order to illustrate structure-activity relationships for the classes of inhibitors tested, each of the 27 inhibitors was docked into homology models of the B. cereus and B. anthracis DHFR proteins, allowing the development of a rationale for the inhibition profiles. A combination of favorable interactions with the diaminopyrimidine and substituted phenyl rings explains the low IC50 values of potent inhibitors; steric interactions explain higher IC50 values. These experiments show that DHFR is a reasonable antimicrobial target for Bacillus anthracis and that there is a class of inhibitors that possess sufficient potency and antibacterial activity to suggest further development.

scholarly journals Hydroxychloroquine in COVID-19 Patients: Pros and Cons

2020 ◽  
Vol 11 ◽  
Author(s):  
Nour K. Younis ◽  
Rana O. Zareef ◽  
Sally N. Al Hassan ◽  
Fadi Bitar ◽  
Ali H. Eid ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Mechanisms Of Action ◽  
Current Evidence ◽  
Therapeutic Effects ◽  
Medical Centers ◽  
Life Threatening ◽  
Pros And Cons ◽  
Neurological Effects

The pandemic of COVID-19, caused by SARS-CoV-2, has recently overwhelmed medical centers and paralyzed economies. The unparalleled public distress caused by this pandemic mandated an urgent quest for an effective approach to manage or treat this disease. Due to their well-established anti-infectious and anti-inflammatory properties, quinine derivatives have been sought as potential therapies for COVID-19. Indeed, these molecules were originally employed in the treatment and prophylaxis of malaria, and later in the management of various autoimmune rheumatic and dermatologic diseases. Initially, some promising results for the use of hydroxychloroquine (HCQ) in treating COVID-19 patients were reported by a few in vitro and in vivo studies. However, current evidence is not yet sufficiently solid to warrant its use as a therapy for this disease. Additionally, the therapeutic effects of HCQ are not without many side effects, which range from mild gastrointestinal effects to life-threatening cardiovascular and neurological effects. In this review, we explore the controversy associated with the repurposing of HCQ to manage or treat COVID-19, and we discuss the cellular and molecular mechanisms of action of HCQ.

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