Pyridazine and its derivative are very important compounds in nitrogen containing heterocyclic compounds due to their various reported pharmacological activities such as antibacterial, muscle relaxant, anti-depressant, antidiabetic, anti-hypertensive, analgesic, anti-tumor, antiviral, nephrotropic, antiinflammatory, anti-viral, anticancer, anti-aggregative, anti-epileptic. It also serves as building block in structure of many chemical constituent of natural compounds phytopharmaceuticals such as cinnolines, phthalazines and also attracting the interest of researchers and medicinal chemist due to its privilege structure which can bear substitution/functionalization easily. Different substituted pyridazine compounds have been synthesized by researchers using different reagents and diverse synthetic route. However most of the investigations available in literature are directed to its large number of biological activities with very less discussion on its various synthetic schemes yielding different type of its derivatives. With the purpose of focusing more on this lack of recent literature this review focuses on different derivative synthesis by using different reaction schemes. Now-a-days pyridazine is serving as ligand in many known chemical reactions and scaffold for drug discovery and development. The aim of this review paper is to encourage more studies on synthesis of pyridazine derivatives which in future will play a vital role for drug discovery.
In the field of molecular modeling, Docking is a method which predicts the preferred orientation of one molecule to a second when bound to each other to form a stable complex. Knowledge of the preferred orientation in turn may be used to predict the strength of association or binding affinity between two molecules. In this study a series of synthesized compounds were evaluated for focusing on binding modes, potential interactions and specific binding sites. Chemically compounds bear both the moiety acyl as well as urea and their interaction by using in silico study was investigated with beta tubulin protein that interferes with the tubulin-microtubule equilibrium, crucial for cellular mitosis. In silico studies revealed that synthesized and tested compounds show 1-7 no. of interactions with amino acids of tubulin protein. Docking study was done by using Autodock, it was found that among different synthesized compound some shows the highest and best scoring pose (lowest energy) which was-2.94 Kcal/mole between N (11) and Leucine (113) and-3.09 between N (11) and Alanine (149). Compounds with amino, hydroxy, methyl, methoxy, trimethoxy and dimethoxy substitution in derivatives of acyl urea gave an idea that urea and acyl when used in combination in different synthesized compounds show good antitumor activity.
Background: 2-pyridone is frequently used to synthesize and develop new bioactive molecules approved for treating many diseases. The produced compounds play a significant role in inhibiting cancer growth. background: : 2-pyridone is frequently used to synthesize and develop new bioactive molecules that have been approved for use in the treatment of many diseases, and the produced compounds play a significant role in the inhibition of cancer growth Objectives: Through a molecular docking investigation, we determined the binding affinity of 2-pyridone compounds with the Matrix Metalloproteinase receptor, which allowed us to develop, produce, and test the in vitro anticancer efficacy of those compounds. objective: Through a molecular docking investigation, we were able to determine the binding affinity of 2-pyridone compounds with the Matrix Metalloproteinase receptor, which allowed us to develop, produce, and test the in-vitro anticancer efficacy of those compounds Method: 2-pyridones (A1-A12) were synthesized in a multistep process, followed by spectrum analysis to confirm the structure. In-silico screening of the synthesized compounds was carried out with the assistance of AutoDock software. Flow cytometry was used on the HT-29 colon cancer cell line to measure A1-A12’s anticancer effect in a lab setting. method: 2-pyridones (A1-A12) were synthesized in a multistep process, followed by their spectrum analysis for confirmation of the structure. In-silico screening of the synthesized compounds was carried out with the assistance of autodock software. Flow cytometry was used on the HT-29 colon cancer cell line to measure A1-A12's anticancer effect in a lab setting Results: The enzyme matrix metalloproteinase receptor and A1-A12 interacted unexpectedly during a docking study (MMP3, MMP9 & MMP13). Research has shown a strong affinity for MMP3 receptors for A9, A10, A11, A12, and A4, respectively. Further flow cytometric testing revealed compound A9 (R1) to be highly cytotoxic, with an IC50 value of 20.77 M. The anticancer activity of A9 (R1) against HT-29 colon cancer cell lines was also confirmed by in vitro results. result: The enzyme matrix metalloproteinase receptor and A1-A12 appeared to interact in an unexpected way during a docking study (MMP3, MMP9 & MMP13). Research has shown a strong affinity for MMP3 receptors for A9, A10, A11, A12, and A4, respectively. Further flow cytometric testing revealed compound A9 (R1) to be highly cytotoxic, with an IC50 value of 20.77 M. The anticancer activity of A9 (R1) against HT-29 colon cancer cell lines was also confirmed by in-vitro results. Conclusion: These findings suggested that 2-pyridone compounds have promising therapeutic potential for cancer treatment, and more research on these lead moieties would be advantageous to discovering an effective anticancer drug. conclusion: These findings suggested that 2-pyridone compounds have promising therapeutic potentials for the treatment of cancer, and more research on these lead moieties would be advantageous to the process of discovering an effective anticancer drug.
Background: Since last decades, breast cancer has emerged as one of the most aggressive form of cancer causing highest mortality rates. The synthetic drugs available for the treatment of breast cancer either have high toxicity or becoming resistant. In view of this, researchers are constantly in search of natural drugs that can control aggressive breast cancer and same time possess less toxicity. Aim: The aim of the manuscript was to summarize potential herbal molecules having significant activity against breast cancer. Methods: Extensive literature survey was carried out to compile data obtained from primary and secondary information sources. Google scholar, science direct, bentham science, springer, pubmed. etc were used as source of data. Result and discussion: In the present review, an attempt has been made to summarize herbal molecules which have shown promising results against breast cancer either in preliminary studies or in clinical studies. Herbal molecules gain good attention among scientific community for their therapeutic properties against breast cancer. Conclusion: After literature survey it was also concluded that herbal molecules have significant potential to control growth of breast cancer.
Background: Anticancer drug development is a tedious process, requiring several in vitro, in vivo, and clinical studies. To avoid chemical toxicity in animals during an experiment, it is necessary to envisage toxic doses of screened drugs in vivo at different concentrations. Several in vitro and in vivo studies have been reported to discover the management of cancer. Materials and Methods: This study has focused on bringing together a wide range of in vivo and in vitro assay methods, developed to evaluate each hallmark feature of cancer. Result: This review provides elaborated information about target-based and cell-based screening of new anticancer drugs in the molecular targeting period. This would help to incite an alteration from the preclinical screening of pragmatic compound-orientated to target-orientated drug selection. Conclusion: Selection methodologies for finding anticancer activity have importance for tumor-specific agents. In this study, advanced rationalization of the cell-based assay is explored along with broad applications of the cell-based methodologies considering other opportunities also.
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