Novel substituted hydrazono indolo[2,1- b ]quinazoline-6,12-dione analogues as cytostatic agents: Synthesis, crystal structure, biological evaluation and molecular docking studies

Novel tryptanthrin hybrids bearing aminothiazoles as potential EGFR inhibitors: Design, synthesis, biological screening, molecular docking studies, and ADME/T predictions

“…Thiazole analogues have attracted considerable attention as potential antitumor agents against various cancer cell lines [21,22]. There have been reports of anticancer [23,24], antimicrobial [25][26][27], antihelmintic [28], antiinflammatory [29], cardiotonic [30], analgesic [31], and antitubercular [32] properties associated with the thiazole moiety. In Figure 1 , the molecule (e) amino thiazole derivative exhibited the strong inhibition activity against EGFR kinase, which was similar to the reference compound erlotinib.…”

Visible Light‐Induced Radical‐Radical Coupling: One‐Pot Synthesis of 6‐Benzyl‐6‐hydroxyindolo[2,1‐b]quinazolin‐12(6H)‐ones from Isatins and Potassium Benzyl Trifluoroborates

“…Tryptanthrin (indolo[2,1‐ b ]quinazoline‐6,12‐dione) and its analogues such as phaitanthrins A−E, 4‐aza tryptanthrin and methylisatoid are important alkaloids isolated from a variety of plants, animals and microorganisms (Figure 1). [3,4] As a class of compounds containing both quinoxalinone and indole backbones, tryptanthrins have unique biological activities, such as antibacterial, antifungal, antiprotozoal and antiparasitic activities, etc [5–7] . Therefore, tryptanthrins are generally considered as important lead compounds for the design of various drug molecules [6] .…”

“…[3,4] As a class of compounds containing both quinoxalinone and indole backbones, tryptanthrins have unique biological activities, such as antibacterial, antifungal, antiprotozoal and antiparasitic activities, etc. [5][6][7] Therefore, tryptanthrins are generally considered as important lead compounds for the design of various drug molecules. [6] Given the scarcity and limitation of tryptanthrins in natural products as well as the considerable value of their unique biological activities, various approaches have been explored to improve the efficiency of constructing this vital skeleton.…”

“…Hz, 1H), 3.37 (d, J = 13.3 Hz, 1H) 13. C NMR (151 MHz, Chloroform-d) δ 160.7 (C=N), 158.2 (C=O), 148.1 (C), 147.5 (C), 144.9 (C), 136.2 (C), 133.7 (C), 132.8 (CH), 130.2 (2CH), 129.7 (CH), 128.2 (2CH), 127.8 (CH), 127.5 (CH), 123.01 (CH), 120.4 (q, J = 260 Hz) (CF 3 ), 120.3 (q, J = 158 Hz) (C), 122.32 (C), 118.0 (CH), 117 7. (CH), 78.7 (C), 46.1 (CH 2 ).…”