Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII

A Series of Isatin-Hydrazones with Cytotoxic Activity and CDK2 Kinase Inhibitory Activity: A Potential Type II ATP Competitive Inhibitor

“…It has been reported that tryptophan obtained from food sources is usually converted to indole by gastrointestinal bacteria, which is further oxidized in the liver by CYP450 to isatin, therefore, isatin is present as an endogenous molecule in humans [ 19 , 20 ]. Various substituents on the isatin nucleus displayed numerous biological activities [ 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 ], including antimicrobial activity[ 31 , 37 ], topoisomerase inhibitory activity [ 7 , 38 ], epidermal growth factor receptor (EGFR) inhibitory activity [ 39 ], inhibitory activities on histone deacetylase (HDAC) [ 40 , 41 ], carbonic anhydrase [ 42 , 43 , 44 ], tyrosine kinase [ 45 , 46 , 47 ], cyclin-dependent kinases (CDKs) [ 9 , 48 , 49 ], adenylate cyclase inhibition [ 50 ] and protein tyrosine phosphatase (Shp2) [ 51 ]. A number of isatin-based marketed drugs and potential anticancer agents [ 41 ] are illustrated in Figure 1 .…”

Synthesis and biological evaluation of certain hydrazonoindolin-2-one derivatives as new potent anti-proliferative agents

“…It is a multikinase inhibitor that targets VEGFR-1, VEGFR-2, PDGFRb, and c-Kit. Recently, our research group has paid much attention to develop many novel small molecules based on the indolin-2-one core as potent anticancer agents [14][15][16][17][18][19][20][21][22] . In 2017, we reported two studies 14,15 regarding development of hydrazonoindolin-2-onebased derivatives and evaluation of their anti-proliferative activity against A549 (lung), HT-29 (colon), and ZR-75 (breast) human cancer cell lines, beside evaluation of their pro-apoptotic activity.…”

“…Based on the aforementioned findings and in connection with our research program on the development of indolin-2-one-based anticancer candidates [14][15][16][17][18][19][20][21][22] , it was thought worthwhile to extend our investigations to probe certain hydrazonoindolin-2-ones displaying promising anti-proliferative activity. In this study, we reported the design and synthesis of different series of hydrazonoindolin-2-ones 3a-e, 5a-e, 7a-c, and 10a-l, adopting three distinctive strategies to develop such derivatives (Figure 2).…”

Isatin-benzoazine molecular hybrids as potential antiproliferative agents: synthesis and in vitro pharmacological profiling

“…In the light of the aforementioned findings and in continuation of our endeavor with respect to the development of potent and effective isatin-based anticancer agents, 35 , 36 we adopted the molecular hybridization approach to design and synthesize four different sets of isatin-quinazolines ( 6a–f and 7a–e )/phthalazines ( 8a–f )/quinoxaline ( 9a–f ) hybrids ( Figure 2 ). All the synthesized hybrids ( 6a–f , 7a–e , 8a–f and 9a–f ) were in vitro evaluated for their antiproliferative activity against three human cancer cell lines, namely human colon cancer HT-29 cell line, breast cancer ZR-75 cell line and lung cancer A-549 cell line.…”