Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents

Antitumour and Acute Toxicity Studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1<em>H</em>)-one Against Ehrlich Ascites Carcinoma and Sarcoma-180

“…chalcones, has been a hot topic [43,44]. The compound under investigation was recently synthesized by a microwave assisted multicomponent strategy and proven to be an antiproliferative agent [28,45,46]. Equal amounts of aromatic ketone (5.0 mmol, 1 eq), aromatic aldehyde (5.0 mmol, 1 eq), urea (5.0 mmol, 1 eq) and 5 mol % of silicated fluoroboric acids catalyst were mixed and placed in a microwave synthesizer for 10 minutes ( In recent years, it happens to be more and more evident that the innovation of novel drugs alone is not satisfactory to make sure the evolution in drug development.…”

Synthesis and antimicrobial evaluation of some 1,2,4-triazolo[1,5-a]pyridine, pyrimidine sulfonamides and sulfinyl derivatives

“…Elemental analyses were carried out at the Microanalytical Center of Cairo University. Ethyl 6-cyano-7-(4-methoxyphenyl)-5-oxo-2-thioxo-1,2,3,5-tetrahydro [1,2,4]triazolo [1,5-a]pyridine-8-carboxylate [48] (1) and 2-(chloromethyl)benzimidazole or 2-(chloromethyl) benzooxazole (2a,b) were prepared according to the reported literature [49][50][51] (Scheme 1).…”

“…Heterocycles containing sulfonamide moieties have attracted obvious attention due to their significant biological properties and their role as pharmacohores [1][2][3][4][5][6]. Studies have shown that sulfonamide compounds were used as antibacterial [7][8][9], antifungal [9,10], antiviral [11], anticancer [12], antinflammatory, analgesic [13][14][15], and antibacterial agents [16].…”

Synthesis of New <i>N</i>¹-Substituted-5-aryl-3-(3,4,5-trimethoxyphenyl)-2-pyrazoline Derivatives as Antitumor Agents Targeting the Colchicine Site on Tubulin

“…They are composed of α and β tubulin heterodimers that are involved in numerous cellular functions including motility, division and intracellular transport. [1][2][3][4][5][6] A number of small molecules bind tubulin interfering with microtubule polymerization and depolymerization, thereby inducing cell cycle arrest leading to apoptosis. It is known that the antitumor efficacy of many chemotherapeutic agents is correlated to their ability to promote apoptosis in cancer cells.…”