854831-80-4Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of some novel 2-pyrazolines bearing benzenesulfonamide as anti-inflammatory and blood glucose lowering agents
Ovais, Syed,Bashir, Rafia,Yaseen, Shafiya,Rathore, Pooja,Samim, Mohammed,Javed, Kalim
, p. 1378 - 1385 (2013)
A series of novel pyrazolines (2a-l) bearing benzenesulfonamide moiety were synthesized by condensing appropriate chalcone (1a-l) with 4- hydrazinobenzenesulfonamide hydrochloride. Structure of all novel synthesized compounds was characterized on basis of
Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation
Moi, Davide,Nocentini, Alessio,Deplano, Alessandro,Balboni, Gianfranco,Supuran, Claudiu T.,Onnis, Valentina
, (2019/08/30)
Four new series of aromatic sulfamates were synthesized and investigated for the inhibition of four human (h) isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), hCA I, II, IX, and XII. The reported derivatives, obtained by a sulfamoylation reaction of the corresponding phenolic precursors, bear 3,5-diarylpyrazoline moieties as spacers between the benzenesulfamate fragment which binds the zinc ion from the active site, and the tail of the inhibitor. Pyrazolines are biologically privileged scaffolds, endowed with versatile biological activity, such as an anti-proliferative action. The derivatives were tested for the inhibition of the cytosolic, hCA I and II (off target isoforms) and the trans-membrane, tumor-associated hCA IX and XII enzymes (anticancer drug targets). Generally, hCA I was not effectively inhibited, whereas many low nanomolar inhibitors were evidenced against hCA II (KIs in the range of 0.42–90.1 nM), IX (KIs in the range of 0.72–63.6 nM), and XII (KIs in the range of 0.88–85.2 nM). The best substitution fragments at the pyrazoline ring included for CA II a 4-sulfamic group on the 3-aryl and halogens on the 5-aryl or a methoxy group on the 3-aryl and a 4-sulfamate group on the 5-aryl; for CA IX and CA XII they included the sulfamic group on the 3- or 4-position of the 5-aryl and an electronwithdrawing group on the 4-postion of the 3-aryl ring.
Design, synthesis, biological evaluation, structure-activity relationship study, and mode of action of 2-phenol-4,6-dichlorophenyl-pyridines
Shrestha, Aarajana,Park, Seojeong,Shin, Somin,Man Kadayat, Tara,Bist, Ganesh,Katila, Pramila,Kwon, Youngjoo,Lee, Eung-Seok
, p. 1 - 18 (2018/05/09)
Human DNA topoisomerases (Topos) are essential nuclear enzyme whose level of expression is potential indicator for prediction of responsive result of chemotherapy. Topos has become a key cellular target for most of the anticancer agents that regulates top
Dihydroxylated 2,6-diphenyl-4-chlorophenylpyridines: Topoisomerase I and IIα dual inhibitors with DNA non-intercalative catalytic activity
Bist, Ganesh,Park, Seojeong,Song, Chanju,Thapa Magar, Til Bahadur,Shrestha, Aarajana,Kwon, Youngjoo,Lee, Eung-Seok
, p. 69 - 84 (2017/04/06)
With the aim to develop novel antiproliferative agents, a new series of eighteen dihydroxylated 2,6-diphenyl-4-chlorophenylpyridines were systematically designed, prepared, and investigated for their topoisomerase (topo) I and IIα inhibitory properties an
Synthesis and biological evaluation of 2-phenol-4-chlorophenyl-6-aryl pyridines as topoisomerase II inhibitors and cytotoxic agents
Thapa, Pritam,Kadayat, Tara Man,Park, Seojeong,Shin, Somin,Thapa Magar, Til Bahadur,Bist, Ganesh,Shrestha, Aarajana,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
, p. 145 - 159 (2016/05/24)
A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU
Synthesis and study of antibacterial and antifungal activities of some new hydroxychalcone-based azo dyes
Baseer, Muhammad,Saeed, Aanier,Samra, Shahid A.,Ashraf, Zaman,Ansari, Farzana L.
, p. 857 - 862 (2013/08/23)
The synthesis of some novel hydroxychalcone azo dyes was accomplished in two steps. The synthetic route involves the base-catalyzed Claisen-Schmidt condensation of suitably substituted benzaldehydes with 3-hydroxyacetophenone in ethanol at room temperatur
