740834-98-4Relevant academic research and scientific papers
Coumarin sulfonamides and amides derivatives: Design, synthesis, and antitumor activity in vitro
Chen, Lexian,Ji, Hong,Li, Guorong,Nie, Minyi,Tan, Yaling,Wang, Zhaohua,Zhang, Jing
, (2021)
Coumarins possesses immeasurable antitumor potential with minimum side effects depending on the substitutions on the basic nucleus, which exhibits great prospects for antitumor drug development. In an attempt to develop novel antitumor candidates, a series of coumarin sulfonamides and amides derivatives were designed and synthetized. The majority of these derivatives showed good cytotoxic activity against MDA-MB-231 and KB cell lines, among which compound 9c was the most potent against MDA-MB-231 cells, with IC50 value of 9.33 μM, comparable to 5-fluorouracil. Further investigation revealed that compound 9c had versatile properties against tumors, including inhibition of cell migration and invasion as well as inducing apoptosis. Reactive oxygen species (ROS) assay and western blotting analysis suggested that compound 9c promoted cancer cell apoptosis by increasing ROS levels and upregulating the expression of caspase-3 in MDA-MB-231 cells. These results indicated that compound 9c could be promising lead compound for further antitumor drug research.
Synthesis and evaluation of antiepileptic activity of newly designed coumarin-sulfonamide hybrids
Dhiman, Neerupma,Gupta, Arti,Kumar, Sandeep,Mallikarjun, B. P.,Sharma, Archana,Singh, Vijay Kumar
, p. 3108 - 3114 (2021/12/14)
The combination of different heterocyclic rings to form a multifunctional compound is a new approach to get the potent and selective compounds, which can act as antiepileptic drugs. In this study we designed and synthesized the hybrid of the coumarin ring with sulfonamide moiety. Coumarin sulfonamide hybrids (CS1-CS7) were synthesized by Knoevenagel condensation of methyl anilinosulfonyl acetate with substituted salicyaldehyde in the presence of catalytic base. The synthesized hybrid compounds were characterized by means of mass, 1H & 13C NMR and FTIR spectroscopy, moreover antiepileptic activity was screened through seizure model of epilepsy using pentylenetetrazole and maximal electroshock. According to results, compound CS-2 remained to be highest potent and presented significant protection at 60 mg/kg in both the seizure models. Furthermore, compound CS-2 was also evaluated for biochemical and a histopathological study in which no significant results were obtained. In addition to former activities, compound CS-2 was also examined for liver toxicity.
Synthesis of new coumarin 3-(N-aryl) sulfonamides and their anticancer activity
Reddy, Natala Srinivasa,Mallireddigari, Muralidhar Reddy,Cosenza, Stephen,Gumireddy, Kiranmai,Bell, Stanley C.,Reddy, E. Premkumar,Reddy, M.V. Ramana
, p. 4093 - 4097 (2007/10/03)
Synthesis of coumarin 3-(N-aryl) sulfonamides was accomplished either by Knoevenagel condensation of anilinosulfonylacetic acids with suitable salicylaldehydes or by the reaction of methyl anilinosulfonylacetates with substituted salicylaldehydes in presence of a catalytic amount of a base. All the compounds tested for antiproliferative activity in different cancer cell lines have shown GI50 values less than 100μM.
