No abstract

Derivatives bearing a specific substitution pattern consisting of 7-phenyl as well as a 2-(4- aminocyclohexylamino) moiety (16c, 16f) display kinase inhibitory activity, elucidated on the basis of molecular simulation studies, which revealed their interaction with the DFG motif of the kinase.

With the aim of enlightening some structure‐activity correlation within the pyranoxanthenone series, we have designed and synthesized a number of new 5‐aminosubstituted pyrano[3,2‐b]xanthen‐6‐ones bearing various 12‐substituents. In vitro cytotoxic potencies of the new derivatives toward the murine leukemia L1210 cell line, human colorectal adenocarcinoma (HT‐29), and human uterine sarcoma (MES‐SA and its 100‐fold resistant to doxorubicin variant MES‐SA/Dx5) cell lines, are described and compared with that of reference drugs. Among the studied compounds, those possessing a second aminosubstituted side‐chain exhibit interesting cytotoxic activity against the solid tumor cell lines, and they retain activity against the multidrug resistant MES‐SA/Dx5 subline. Their selective effect on a phase of the cell cycle was evaluated using HT‐29 cells providing evidence that the compounds induce a G0/G1 arrest. J. Heterocyclic Chem., (2011).

A number of new aminosubstituted benzofuran analogues have been prepared and their cytotoxic/cytostatic activity was investigated against five human tumor cell lines (MCF-7, SKBR3, SKOV3, HCT-116 and HeLa). Certain compounds showed noticeable tumor cell growth inhibition, indicative of possible structure-activity relationships.

Design, Synthesis, and Cytotoxic Activity Evaluation of New Linear Pyranoxanthone Aminoderivatives. -The hydrochlorides of the compounds (IV), the free amines (VIII) and (XIIIa), and the difumarate of the compound (XIIIb) are screened for their in vitro cytotoxicity against the murine leukemia L1210 cell line, human colorectal adenocarcinoma (HT-29), and human uterine sarcoma (MES-SA and the multidrug resistant variant MES-SA/Dx5) cell lines in comparison to the reference drugs mitoxantrone and doxorubicin. In general, the compounds (VIII) and (XIII) show more activity against the tested cell lines than the compounds (IV). Interestingly, all compounds show a higher activity against the MES-SA/Dx5 cell line than against the MES-SA cell line. -(KOLOKYTHAS, G.; DANIILIDES, K.; POULI, N.; MARAKOS*, P.; PRATSINIS, H.; KLETSAS, D.; J. Heterocycl. Chem. 48 (2011) 4, 927-935, http://dx.