Pharmaceutical Sciences and Natural Products - Research Publications

Permanent URI for this collectionhttps://kr.cup.edu.in/handle/32116/56

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Author: search.filters.author.Ansari, Arshad J.

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    FDA approved fused pyrimidine-based drugs
    (Elsevier, 2022-10-14T00:00:00) Thakur, Shikha; Ansari, Arshad J.; Joshi, Gaurav
    The present chapter is a compilation and analysis of USFDA approved small drug candidates about fused pyrimidine pharmacophore. Out of 63 drugs approved so far, nearly 38% of drugs are approved for chemotherapeutic treatment of cancer. Further, antiviral category shares 19% followed by drugs for cardiovascular disorders (14%), inflammatory diseases (9%), respiratory disorders (6%), neurological disorders (5%), benign prostatic hypertrophy (3%), erectile dysfunction (2%), diabetes (2%) and thrombocytopenia (2%). The chapter further focuses on key biological targets affected by the reported drug and their pharmacological mechanism of action. We have also focused on elucidating key chemical taxonomy utilized in fused pharmacophores of pyrimidine. The analysis suggested purine nucleosides (11 drugs) and xanthines/hypoxanthines (11 drugs) share the major chunk utilized in drug development out of fused pyrimidine nucleus. � 2023 Elsevier Ltd. All rights reserved.
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    Design, synthesis and anticancer activity of 2-arylimidazo[1,2-a]pyridinyl-3-amines
    (Academic Press Inc., 2021-11-01T00:00:00) Yadav, Umesh Prasad; Ansari, Arshad J.; Arora, Sahil; Joshi, Gaurav; Singh, Tashvinder; Kaur, Harsimrat; Dogra, Nilambra; Kumar, Raj; Kumar, Santosh; Sawant, Devesh M.; Singh, Sandeep
    A series of imido-heterocycle compounds were designed, synthesized, characterized, and evaluated for the anticancer potential using breast (MCF-7 and MDA-MB-231), pancreatic (PANC-1), and colon (HCT-116 and HT-29) cancer cell lines and normal cells, while normal cells showed no toxicity. Among the screened compounds, 4h exhibited the best anticancer potential with IC50 values ranging from 1 to 5.5 ?M. Compound 4h caused G2/M phase arrest and apoptosis in all the cell lines except MDA-MB-231 mammosphere formation was inhibited. In-vitro enzyme assay showed selective topoisomerase II? inhibition by compound 4h, leading to DNA damage as observed by fluorescent staining. Cell signalling studies showed decreased expression of cell cycle promoting related proteins while apoptotic proteins were upregulated. Interestingly MDA-MB-231 cells showed only cytostatic effects upon treatment with compound 4h due to defective p53 status. Toxicity study using overexpression of dominant-negative mutant p53 in MCF-7 cells (which have wild type functional p53) showed that anticancer potential of compound 4h is positively correlated with p53 expression. � 2021 Elsevier Inc.
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    Exploring the magic bullets to identify Achilles� heel in SARS-CoV-2: Delving deeper into the sea of possible therapeutic options in Covid-19 disease: An update
    (Elsevier Ltd, 2020-11-27T00:00:00) Thakur, Shikha; Mayank; Sarkar, Bibekananda; Ansari, Arshad J.; Khandelwal, Akanksha; Arya, Anil; Poduri, Ramarao; Joshi, Gaurav
    The symptoms associated with Covid-19 caused by SARS-CoV-2 in severe conditions can cause multiple organ failure and fatality via a plethora of mechanisms, and it is essential to discover the efficacious and safe drug. For this, a successful strategy is to inhibit in different stages of the SARS-CoV-2 life cycle and host cell reactions. The current review briefly put forth the summary of the SARS-CoV-2 pandemic and highlight the critical areas of understanding in genomics, proteomics, medicinal chemistry, and natural products derived drug discovery. The review further extends to briefly put forth the updates in the drug testing system, biologics, biophysics, and their advances concerning SARS-CoV-2. The salient features include information on SARS-CoV-2 morphology, genomic characterization, and pathophysiology along with important protein targets and how they influence the drug design and development against SARS-CoV-2 and a concerted and integrated approach to target these stages. The review also gives the status of drug design and discovery to identify the drugs acting on critical targets in SARS-CoV-2 and host reactions to treat Covid-19. � 2020 Elsevier Ltd