Design, Synthesis and Antitumor Activity Evaluation of 1,3,4-Thia-diazole, Thioether and Amide Based 1,3-Disubstituted-indol-2-one Derivatives

Recent advances in isatin hybrids as potential anticancer agents

“…Hybrids 37 (IC 50 : 1.61–25.46 μM, MTT assay) with 1,3,4‐thiadiazole backbone at the N‐1 position of isatin moiety showed potential activity against HepG2, AsPc‐1, and HeLa cancer cell lines and the activity was no inferior to that of the reference gefitinib (IC 50 : 5.19–16.41 μM). [ 91 ] Hybrids 38 (IC 50 : 10.46–21.41 μM, MTT assay) with 1,3,4‐thiadiazole backbone at C‐3 position of isatin moiety also showed considerable activity against MCF‐7 cancer cells and the SAR implied that introduction of alkyl or benzyl group into N‐1 position of isatin motif or incorporation of electron‐withdrawing group into phenyl ring (R 2 position) had little impact on the activity. [ 92 ] The isatin–1,3,4‐thiadiazole hybrids 39 were active against a panel of 60 human cancer cell lines derived from nine different cancer types: leukemia, lung, colon, central nervous system (CNS), melanoma, ovarian, renal, prostate, and breast; hybrids 39a,b (IC 50 : 0.65–17.09 μM, MTT assay) possessed broad‐spectrum activity against the tested cancer cell lines.…”

Synthesis and Antitumor Activity of Amide Derivatives Containing 1,3,4-Thiadiazole and Pyrazole Moieties

“…Nitrogen-containing heterocycles compounds possessing 1,3,4-thiadiazole and pyrazole functional groups usually exhibit unique physiological and pharmacological properties. [1][2][3][4][5][6] For example, 1,3,4-thiadiazole compounds exhibit a broad range of novel biological activities such as antiinflammatory, [7][8] antibacterial, [9][10][11] antiviral, [12] prevent depression, [13] anticonvulsant [14] and anticancer [15][16][17][18][19] activi-ties. Pyrazole derivatives are of great importance in the field of pesticides and medicinal chemistry such as insecticidal activity, [19] anti-inflammatory, [20][21] anti-tuberculosis, [22][23] antifungal, [24][25] antiviral, [26][27][28] anticancer [29][30][31][32][33] activities.…”

Novel 3-Thioether-4-indolimino-4H-1,2,4-triazole Derivatives Bearing Pyridyl Moiety: Design, Synthesis and Bioactivity Evaluation in vitro

“…[6] The amino and mercapto groups are ready-made nucleophilic centers for the preparation of fused heterocyclic rings. [21] Noteworthily, our previous work led to the discovery of a series of novel substituted indole derivatives possessing excellent antitumor activities, such as compounds 4, [22] 5 [23] (Figure 1) and antimicrobial activities [24] such as compound 6 [25] (Figure 1). Moreover, there are also many drugs containing indole moiety for tumor treatment, such as nintedanib, vinblastine, vinorelbine, sunitinib, melatonin, indirubin, etc.…”