The antitumor activity of novel pyrazoloquinoline derivatives

Design, Synthesis and Anticancer Screening of Novel Pyrazole Derivatives Linking to Benzimidazole, Benzoxazole and Benzothiazole

“…Benzothiazole derivatives were reported to show growth inhibition against a broad spectrum of human cancer cells and induced apoptosis of HepG2 cells in a dose- and time-dependent manner [27,28]. In addition, pyrazole nucleus was revealed to have an important role in producing anti-tumor potencies [13,29]. Based on these reports, the linking pyrazole derivatives to benzimidazole, benzoxazole and benzothiazole in the present study may potentiate the anti-tumor efficacies of novel pyrazol-3-ylamine and pyrazole-3,5-diamine derivatives.…”

“…Through searching in the literature, it was found that benzothiazole derivatives play an important role on designing of new drugs, since they present an interesting pharmacological profile [3], including anti-allergic [4], anti-inflammatory [5], antitumor [6], analgesic [7], antimicrobial [8,9], anthelmintic [10], antileishmanial [11], anticonvulsant [12] activities, also with considerable efficacy as kinase, topoisomerase I/II and transretinoic acid metabolism inhibitors [1]. In addition, pyrazole nucleus is an important pharmacophore with a wide range of therapeutically activities such as antitumor [13], antibacterial, anti-inflammatory [14] and hypotensive [14] efficacies and also acts as ligands for benzodiazepine receptors [15]. In addition, benzoxazole or benzimidazole have variable pharmacological activities like antitubercullosis [16], antioxidant, anthelmintic [17], antimicrobial [18] and anticancer [19] potentials.…”

Synthesis and biological activity of pyrimido [1, 2-a] quinoline moiety and its 2-substituted derivatives

“…Despite its relatively low efficacy and tolerability, quinine still plays an important role in the treatment of multi resistant malaria 1 . Quinoline and its derivatives are receiving important due to their due to wide range of biological activities as a drug analgesics 2 ,antiamoebic [3][4][5][6] , tryphocidal 7 , antiseptic 8 and antiserotonin 9 .In addition to these, derivatives also exhibit good antimalarial 10,11 , antitubercular 12 , antibacterial 13 , antihistaminic 14 , antineurodegerative 15 , anticonvulsant 16 , antitumor 17 , anticancers [18][19][20] and antiallergics 21 activities. In view of these observations, such as quinoline fused with pyrimidine ring would exhibit some interesting pharmacological activities, further, the ring anellation to amino groups containing nitrogen heterocycles with ketene dithioacetals as reagent has reported [22][23] .…”

Synthesis and Antimicrobial Activity of 3‐Cyano‐4‐imino‐9‐methoxy‐4H‐pyrimido [2, 1-b] pyrimido [4, 5-b] quinoline and 2‐Substituted Derivatives

“…Quinoline and its derivatives are receiving important due to their wide range of biological activities as a drug analgesics [4], antiamoebic [5][6][7][8], trypanocidal [9], antiseptic [10], and antiserotonin [11]. In addition to these, derivatives also exhibit good antimalarial [12,13], antitubercular [14], antibacterial [15], antihistaminic [16], anti-neurodegerneative [17], anticonvulsant [18], antitumor [19], anticancers [20,21], and antiallergics [22] activities.…”