Design, Synthesis and Evaluation of Core Scaffold Pyrazolone Fused Thiazolidinone Derivatives as Anticancer Agents

نویسندگان

چکیده

Background: Cancer is the world's second leading cause of death, accounting for an estimate more than 10 million deaths annually. The most common type cancers in women are breast, endometrial, cervical, ovarian, colorectal, lung, and skin cancers.Among these, breast cancer all ages. Human epidermal growth factor receptor 2 widely seen which test positive protein HER2. This present one-fifth every cell, promotes cells. There several compounds available treatment HER2 market with varying promise their efficacy safety on treatment.
 Objective: To design synthesis evaluation core scaffold pyrazolone fused thiazolidinone derivatives as anticancer agents.
 Methods: In this study, were designed, synthesized, analyzed activity using carcinoma cell line (MCF-7), against standard drug Doxorubicin.
 Results: Many thiazoles, thiazole, pyrazole have been found to anti-cancer other properties. compound 1-phenyl-3-methyl-5-pyrazolones was allowed react diverse benzoyl chloride well primary amine transformed into ’A series Pyrazolone Thiazolidinone 4A1-4A10 4B1- 4B10. Computational studies by Schrodinger Glide XP Protein 3RCD act human receptor’’ performed selected scheme initially further from docked score data performed.
 Conclusion: Among five (4A6 ? 3.4 kcal/mol, 4B4 3.0 4A3 2.2 4B2 1.6 4A9 1.3 kcal/mol) shown promising binding affinities kinase. cytotoxic potential examined a cytotoxicity close Doxorubicin (standard drug). Our findings important step forward development novel agents.

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ژورنال

عنوان ژورنال: Journal of pharmaceutical research international

سال: 2021

ISSN: ['2456-9119']

DOI: https://doi.org/10.9734/jpri/2021/v33i31b31710