Abstract:The reaction of 3‐(1,4‐dioxo‐3,4‐dihydrophthalazin‐2(1H)‐yl)‐3‐oxopropanenitrile 1 and salicyladehyde furnished coumarin derivatives 4 and 5. Coupling reaction of 1 with aryl diazonium chlorides and benzene‐1,4‐bis (diazonium) chloride gave the corresponding hydrazones 6a,b and bishydrazone 9, respectively. Hydrazones 6 underwent intramolecular cyclization upon treating with hydrazine hydrate to give 3‐aminopyrazoles 7. Pyranyl phthalazine 13 was prepared from the reaction of 1 with ethyl 2‐cyano‐3‐ethoxyacryl… Show more
“…In addition, Sulfonyl or sulfonamide hybrids were broadly explored for their anticancer activities via different mechanisms [8][9][10][11][12][13][14][15][16][17] and it was found that they possess minimum side effects along with multi-drug resistance activity. Therefore, and in continuation of our interest to develop a series of novel small molecules as potential antitumor agents that can block biologically relevant molecular targets [18][19][20][21][22] , we prepared certain pyrazoles, pyridines, thiazoles derivatives containing sulfonamide pharmacophores and studied their activity against breast cancer cell line (MCF-7).…”
Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer. New series of pyrazole, pyridine, thiazole derivatives containing sulfonamide moiety were prepared and screened for their antitumor activity against breast cancer cell line (MCF-7). The results of this investigation revealed that compounds 3 and 8 had signi cant anticancer activity against the MCF-7 cancer cell line with IC50 values 19.2 and 14.2 μM, respectively, in relation to the standard drug, doxorubicin.
“…In addition, Sulfonyl or sulfonamide hybrids were broadly explored for their anticancer activities via different mechanisms [8][9][10][11][12][13][14][15][16][17] and it was found that they possess minimum side effects along with multi-drug resistance activity. Therefore, and in continuation of our interest to develop a series of novel small molecules as potential antitumor agents that can block biologically relevant molecular targets [18][19][20][21][22] , we prepared certain pyrazoles, pyridines, thiazoles derivatives containing sulfonamide pharmacophores and studied their activity against breast cancer cell line (MCF-7).…”
Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer. New series of pyrazole, pyridine, thiazole derivatives containing sulfonamide moiety were prepared and screened for their antitumor activity against breast cancer cell line (MCF-7). The results of this investigation revealed that compounds 3 and 8 had signi cant anticancer activity against the MCF-7 cancer cell line with IC50 values 19.2 and 14.2 μM, respectively, in relation to the standard drug, doxorubicin.
“…Compounds containing the pyridine pattern have a wide range of biological profiles including antimicrobial 31 – 36 , anti-viral 37 , 38 , antioxidant 39 , antidiabetic 40 , anticancer 41 – 43 , anti-inflammatory agents 44 , 45 . For all these benefits related to thiazole and pyridine derivatives and following our work 46 – 50 , we report here the synthesis of a new library of thiazole derivatives from 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2 H )-yl)thiourea 2 . Figure 2 Structure of amrinone and milrinone.…”
A novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline, respectively. The potential DNA gyrase inhibitory activity was examined using in silico molecular docking simulation. The novel thiazoles exhibit dock score values between − 6.4 and − 9.2 kcal/mol and they were screened for their antimicrobial activities. Compound 13a shown good antibacterial activities with MIC ranged from 93.7–46.9 μg/mL, in addition, it shown good antifungal activities with MIC ranged from 7.8 and 5.8 μg/mL.
“…In addition, Sulfonyl or sulfonamide hybrids were broadly explored for their anticancer activities via different mechanisms [8][9][10][11][12][13][14][15][16][17] and it was found that they possess minimum side effects along with multi-drug resistance activity. Therefore, and in continuation of our interest to develop a series of novel small molecules as potential antitumor agents that can block biologically relevant molecular targets [18][19][20][21][22] , we prepared certain pyrazoles, pyridines, thiazoles derivatives containing sulfonamide pharmacophores and studied their activity against breast cancer cell line (MCF-7).…”
Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer. New series of pyrazole, pyridine, thiazole derivatives containing sulfonamide moiety were prepared and screened for their antitumor activity against breast cancer cell line (MCF-7). The results of this investigation revealed that compounds 3 and 8 had significant anticancer activity against the MCF-7 cancer cell line with IC50 values 19.2 and 14.2 μM, respectively, in relation to the standard drug, doxorubicin.
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