Rui-Qing Wang

New class of potent antitumor acylhydrazone derivatives containing furan.

A pair of chemical isomeric structures of N-acylhydrazone compounds I and II were designed and synthesized. The reaction was carried out with high diastereoselectivity to obtain one configurational isomer in excellent yields. The exact configuration and conformation of IIa and IIe were confirmed by the X-ray single crystal diffraction. The antitumor bioassay revealed that some compounds exhibited excellent activity against the selected cancer cell lines. In particular, IIf (IC50=16.4 μM) was better than doxorubicin (IC50=53.3 μM) against human promyelocytic leukemic cells (HL-60). Their toxicities were predicted in silico. The results showed that compounds II were safe and eligible to be development candidates. IIf showed great promise as a novel lead compound for further anticancer discovery.

Cytotoxic activity of some Asarum plants.

The cytotoxic activity against some tumor cell lines of 16 commonly used species of Asarum was evaluated in this study. All of these plants were widely used in Asian countries as traditional medicines or folk medicines. Their inhibitory activities against four tumor cell lines (HL-60, BGC-823, KB and Bel-7402) were compared. It was observed that 10 of the tested extracts (eight ethanol extracts and two water extracts) among 32 extracts of these plants showed cytotoxic activity. Those 95% ethanol extractions from A. caudigerellum, A. forbesii, A. inflatum and A. maximum exhibited the highest cytotoxic activity, and 95% ethanol extracts or water extracts of A. sieboldii var. seoulense, A. himalaicum, A. splendens and A. crispulatum showed selective activity against one or two cells among the tested tumor cells. This is the first report of Asarum plants possessing cytotoxic activity against tumor cell lines.

SYNTHESIS, SPECTROSCOPIC CHARACTERIZATION, AND IN VITRO ANTITUMOR ACTIVITY OF TETRAPHENYLANTIMONY DERIVATIVES OF ANALOGUES OF DEMETHYLCANTHARIDIN AND DEMETHYLDEHYDROGEN-CANTHARIDIN

ABSTRACT A series of novel tetraphenylantimony(V) derivatives of the analogues of demethylcantharidin and demethyldehydrogencantharidin, exo-7-oxa-bicyclo[2,2,1]-heptane-3-arylamide-2-carboxylic acid and exo-7-oxa-bicyclo[2,2,1]-heptene-3-arylamide-2-carboxylic acid, of the general formulas , , , and have been synthesized and characterized by elemental analyses, IR, 1H NMR and mass spectroscopy. Preliminary antitumor activity tests show that these compounds have significant antitumor activity in vitro against five human neoplastic cell lines.

Synthesis, cytotoxicity and DNA-binding levels of new type binuclear platinum(II) complexes.

Six new type binuclear platinum(II) complexes (a-f) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, (1)H NMR and mass spectra techniques. The cytotoxicity of the complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS, respectively. The results indicate that the complex (a) has no cytotoxicity against HL-60, BGC-823, Bel-7402, KB and Hela, the complexes (b, c, e and f) have weaker cytotoxicity against some tested carcinoma cell lines, the complex (d) has better cytotoxicity against HL-60, BGC-823, Bel-7402, KB, MCF-7, HCT-8 and Hela with respect to the IC(50) values obtained. The cytotoxicity of the complex (d) is equal to that of cisplatin against HL-60 and Bel-7402 (P>0.05), but it has better cytotoxicity than that of cisplatin against BGC-823 and MCF-7 (P<0.05). The complex (d) causes significant G(2)/M arrest and a concomitant decrease of cell population in G(1) and S phases, and the total DNA platination levels of the complex (d) are higher than those of cisplatin under the same experimental conditions. It suggests that the bridging linker has important effect on their cytotoxicity. Indeed, when the bridging linker is dicarboxylic acid, their cytotoxicity is better than that of platinum complexes with an amino acid as bridging linker. The new type binuclear platinum(II) complexes represent a novel class of anticancer agents, which deserves further attention in search of anticancer lead compounds.