Abstract
Pyrazoles, thiazoles and fused thiazoles have been reported to possess many biological activities. 3-Methyl-5-oxo-4-(2-arylhydrazono)-4,5-dihydro-1H-pyrazole-1-carbothioamides 3a,b (obtained from the reaction of ethyl 3-oxo-2-(2-arylhydrazono)butanoates 1a,b with thiosemicarbazide) could be transformed into a variety of thiazolyl-pyrazole derivatives 6a–h, 10a–c, 15a–c, 17, 19 and 21 via their reaction with a diversity hydrazonoyl chlorides as well as bromoacetyl derivatives. Moreover, the computational studies were carried out for all new compounds. The results indicated that five compounds showed promising binding affinities (10a: − 3.4 kcal/mol, 6d: − 3.0 kcal/mol, 15a: − 2.2 kcal/mol, 3a: − 1.6 kcal/mol, and 21: − 1.3 kcal/mol) against the active site of the epidermal growth factor receptor kinase (EGFR). The cytotoxicity of the potent products 3a, 6d, 10a, 15a, and 21 was examined against human liver carcinoma cell line (HepG-2) and revealed activities close to Doxorubicin standard drug. There was an understanding between the benefits of restricting affinities and the data obtained from the practical anticancer screening of the tested compounds.
Highlights
The pyrazole nucleus has many biological activities, including several pharmaceuticals currently on the market
Drug design part guarantees that thiazole is best particle for the said target activity
To avoid interference of the active methylene in the following reactions ethyl acetoacetate was coupled with aryl diazonium salts to afford the hydrazo derivatives 1a,b; which are the starting compounds for the synthesis of target thiazolyl-pyrazole derivatives
Summary
The pyrazole nucleus has many biological activities, including several pharmaceuticals currently on the market. Pyrazole derivatives have found numerous applications in fluorescent substances, dyes, agrochemicals, and more. Thiazoles are significant class of heterocyclic compounds, found in numerous powerful biologically active drugs such as Ritonavir (antiretroviral drug), Sulfathiazole (antimicrobial drug), Tiazofurin (antineoplastic drug), and Abafungin (antifungal drug) [7]. Compounds containing thiazole show many biological activities such as Thiazole derivatives are known to possess several anticancer activities [13,14,15]. Thiazoles have better action as an anticancer just as it demonstrates better binding domain and they have less cytotoxicity to normal cell (physiological cell) alongside that it has site explicit movement to malignant growth cell (pathological cell). We can seek after the superior to best treatment for malignant growth
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