Synthesis, characterization, and pharmacological evaluation of some novel thiadiazoles and thiazoles incorporating pyrazole moiety as anticancer agents

Ethyl 7-Methyl-1-(4-nitrophenyl)-5-phenyl-3-(thiophen-2-yl)-1,5-dihydro-[1,2,4]triazolo[4,3-a]pyrimidine-6-carboxylate

“…The 13 C-NMR spectrum provided the expected number and types of carbons. It showed five characteristic signals at δ = 13.8 (CH 3 Encouraged by the above observations and in continuation of our previous work on the synthesis of antitumor agents [17][18][19][20][21], the synthesis of a 1,2,4-triazolopyrimidine, incorporating the thiophene moiety as a promising antitumor agent, was planned, using N-(4-nitrophenyl)thiophene-2-carbohydrazonoyl chloride as a versatile building block.…”

“…Encouraged by the above observations and in continuation of our previous work on the synthesis of antitumor agents [17][18][19][20][21], the synthesis of a 1,2,4-triazolopyrimidine, incorporating the thiophene moiety as a promising antitumor agent, was planned, using N-(4-nitrophenyl)thiophene-2-carbohydrazonoyl chloride as a versatile building block. the growth of a wide range of cancer cell lines including leukemia and prostate and lung cancer at low dose levels [15].…”

Synthesis, Characterization and Molecular Docking of Novel Bioactive Thiazolyl-Thiazole Derivatives as Promising Cytotoxic Antitumor Drug

“…Thiazoles are a familiar group of heterocyclic compounds possessing a wide variety of biological activities, and their usefulness as medicines are well established. Thiazole derivatives are reported to exhibit diverse biological activities as antimicrobial [3][4][5], antioxidant [6], antitubercular [7], and anticonvulsant [8], and anticonvulsant, anticancer [9,10] agents. Moreover, many derivatives of thiazoles are used as selective Cyclooxygenase-2 Inhibitors [11], in addition to their use as 5-HT3 receptor antagonists [12] and as potent and selective acetyl Co-A carboxylase-2 inhibitors [13].…”

“…As a part of our research interest towards developing new routes for the synthesis of a variety of heterocyclic systems with promising antitumor activities [9,10,[16][17][18][19][20][21][22], we report in the present work the synthesis of a new series of thiazolyl-thiazoles as promising cytotoxic antitumor drugs.…”

Synthesis of New 3-Heteroarylindoles as Potential Anticancer Agents

“…The 1,2,4-triazolopyrimidines have also attracted growing interest due to their important pharmacological activities, such as antitumor, antimalarial, antimicrobial, anti-inflammatory, and antifungal activity, as well as macrophage activation [17][18][19][20][21][22]. 1,3,4-Thiadiazole derivatives have attracted considerable interest owing to their wide ranging biological activities such as antibacterial, antifungal, antituberculosis, antihepatitis B viral, antileishmanial, anti-inflammatory, analgesic, CNS depressant, anticancer, antioxidant, antidiabetic, molluscicidal, antihypertensive, diuretic, analgesic, antimicrobial, antitubercular, and anticonvulsant activities [23][24][25][26][27][28][29][30][31][32]. In light of these facts, we have synthesized some new thiazole, dihydropyrido [3,2-e] [1,2,4]triazolo [4,3-a]pyrimidine and 1,3,4-thiadiazole derivatives using 3-acetylindole as a common precursor and screened these compounds for their anticancer activities.…”