Design, synthesis and biological evaluations of novel pyridone-thiazole hybrid molecules as antitumor agents

Organocatalyzed Domino Synthesis of New Thiazole‐Based Decahydroacridine‐1,8‐diones and Dihydropyrido[2,3‐d : 6,5‐d′]‐ dipyrimidines in Water as Antimicrobial Agents

“…Thiazole ring is a structural fragment of natural compounds such as thiamine (vitamin B1), thiamine pyrophosphate, epothilones, carboxylase, and the large family of macrocyclic thiopeptide antibiotics, thiostrepton and micrococcin P1 . Thiazole derivatives are associated with a broad spectrum of biological properties, including anticancer, antitumor, anticonvulsant, antimicrobial, antituberculous and bacteriostatic activities ( Figure ) . Therefore, we focused on attention to club theses heterocycles in one molecular framework to synthesize new hybrids thiazolyl acridinedione.…”

“…[24,25] Thiazole derivatives are associated with a broad spectrum of biological properties, including anticancer, antitumor, anticonvulsant, antimicrobial, antituberculous and bacteriostatic activities (Figure 1). [26][27][28][29] Therefore, we focused on attention to club theses heterocycles in one molecular framework to synthesize new hybrids thiazolyl acridinedione.…”

Synthesis, Spectral Characterization and Pharmacological Evaluation of Novel Thiazole-Oxoindole Hybrid Compounds as Potential Anticancer Agents

“…1 H NMR spectrum (DMSO-d 6 ) exhibited two singlet signals at δ 9.42 and 11.61 ppm assignable to two NH, in addition to a multiplet signal at δ 7.10-7.81 ppm distinctive for aromatic protons. In addition, 13 C NMR spectrum of 4c displayed signals at δ 46.34 and 65.67 ppm for CH 2-morpholinyl , also two signals were observed at 154.17 and 168.89 ppm corresponding to the two carbonyl groups. Also, treatment of (1) with 2-(4-oxo-2thioxothiazolidin-3-yl) acetic acid produces 2- (5-(5-(morpholinosulfonyl)-2-oxoindolin-3ylidene)-4-oxo-2-thioxothiazolidin-3-yl) acetic acid (5) based on elemental analysis and spectral data.…”

“…The 1 H NMR spectrum (DMSO-d 6 ) exhibited two singlet signals at δ 3.81, 6.77 due to methoxy and -CH methine exocyclic as well as two singlet signals due to two NH at 11.27, 11.64 ppm in addition to the morpholinyl and aromatic protons. Also, 13 C-NMR spectrum showed presence of morpholinyl, methoxy, aromatic and methine carbons at 46. 21 In addition, 3-(2-(4-arylthiazol-2-yl) hydrazono)-5-(morpholinosulfonyl)indolin-2ones (12a-c) were produced through alkylation of the thiosemicarbazone derivative (10) with phencylbromides in acetic acid containing sod.acetate.…”

“…Thiazoles are one of the most intensively investigated classes of aromatic five membered heterocycles and immense attention because it used as building block for the synthesis of many biologically active molecules as Sulfathiazole (antimicrobial drug), Nitazoxanide (antiprotozoal agent), Nizatidine (ulcer therapeutic), Abafungin (antifungal drug), Tiazofurin (antineoplastic agent), Meloxicam (non-steroidal, anti-inflammatory drug), epothilones and Antiarrhythmic, Anticoagulant activities [3][4][5][6][7][8] as shown in figure (1). Also, some natural products containing thiazole ring have been isolated as thiamine (vitamin B1), thiamine pyrophosphate (TPP, a coenzyme important in respiration in the Krebs cycle) [9,10] and most of them exhibited significant cytotoxicity and antitumor potential [11][12][13]. Thus, the thiazole nucleus has been much studied in the field of organic and medicinal chemistry.…”