Aurora Molinari

Cytotoxic–antineoplastic activity of hydroquinone derivatives

Several myrcenylhydroquinone derivatives have been evaluated for their cytotoxic activity against three neoplastic cell line cultures and compared with the activity previously observed on other neoplastic systems. Also a new series of this type of compounds has been prepared and the compounds synthesised have been evaluated by their GI(50) values.

New antineoplastic prenylhydroquinones. Synthesis and evaluation.

Several prenylhydroquinones have been prepared through Diels-Alder condensation, further functionalized or degraded chemically and then evaluated for their cytotoxic activity against some neoplastic cultured cell lines. A number of them have shown IC50 values under the microM level.

Diterpenes from Calceolaria latifolia

Abstract Four new diterpene compounds have been isolated from the aerial parts of Calceolaria latifolia , and their structures elucidated by spectroscopic methods. Two of them present a pimaradiene type skeleton and the other two, a stemarane skeleton.

Synthesis and Cytotoxic Evaluation of 6-(3-Pyrazolylpropyl) Derivatives of 1,4-Naphthohydroquinone-1,4-diacetate

Several new 6‐(3‐pyrazolylpropyl) derivatives of 1,4‐naphthohydroquinone‐1,4‐diacetate (NHQ‐DA) have been prepared by chemical modifications of the Diels–Alder adduct of α‐myrcene and 1,4‐benzoquinone. All these new compounds and precursors have been evaluated in vitro for their cytotoxicity against cultured human cancer cells of MB‐231 breast‐adeno carcinoma, A‐549 lung carcinoma, and HT‐29 colon carcinoma. GI50 values ranged in and below the micromolar concentration level.

A New Application of Dimethyl Trithiocarbonate. Methylthiothiocarbonylation of 2,4-Pentanedione and Some β-Oxoesters

Abstract 2,4-Pentanedione, ethyl acetoacetate, benzoyl acetate and diethyl malonate 1a-d react with sodium acetate and dimethyl trithiocarbonate in dimethylformamide to afford methyl-β,β′-dicarbonyldithiocarboxylate derivatives 2a-d in moderate yield.

A stemarane diterpene from Calceolaria kingii

Abstract The aerial parts of Calceolaria kingii yielded a new stemarane diterpene. Its structure was deduced on the basis of spectral data.

2,3-FUNCTIONALLY DIALKYL-1,4-BENZOHYDROQUINONE DIACETATE DERIVATIVES FROM CLEAVAGE OF EPOXIDES

Se han preparado una serie de nuevos compuestos del tipo diacetatos de 1,4-benzohidroquinona-2,3-dialquilsustituidos, por oxidacion degradativa de epoxidos III, obtenidos del producto de condensacion Diels-Alder entre el monoterpeno mirceno y la 1,4-benzoquinona. La naturaleza de los productos aislados depende de los grupos funcionales presentes en las cadenas alquilicas

Cytotoxic‐Antineoplastic Derivatives of Prenyl‐1,2‐naphthohydroquinone

Several new prenyl‐1,2‐naphthohydroquinone derivatives have been prepared by chemical modifications of Diels–Alder products which were obtained from cycloaddition of α‐myrcene to 1,2‐benzoquinone and then evaluated in vitro for their cytotoxic activity against A‐549 lung carcinoma, HT‐29 colon carcinoma, and MB‐231 breast adeno‐carcinoma culture cells. Most of them exhibited GI50 values in the μM‐concentration level.

Electrochemical study of some three-derivative compounds of 1-phenyl-4-butyldithiocarboxylate-5-hydroxypyrazol (3D-FBDTCHP)

An electrochemical study related to the electrooxidation of the 3-hydroxyl and 3-methyl derivatives of 1-phenyl-4-butyldithiocarboxylate-5-hydroxypyrazol in aqueous ethanolic solutions covering a wide pH interval has been performed. In this study, these compounds are considered as potential collector agents for copper mineral sulfide flotation. From the potentiodynamic parameters for both compounds in solution, as well as for the 3-methyl derivative adsorbed on a glassy carbon electrode surface, it was established that these compounds undergo a dimerization process involving the formation of the respective bisthiocarbonyl disulfide derivative. On the basis of the voltammetric and coulometric data, as well as from the analysis of the product obtained after a preparative electrolysis carried out with the 3-methyl derivative, a mechanism accounting for the nature of the reaction product in aqueous ethanolic solutions is proposed.

New 1H-Benzo[f]indazole-4,9-diones Conjugated with C-Protected Amino Acids and Other Derivatives: Synthesis and in Vitro Antiproliferative Evaluation.

1H-Benzo[f]indazole-4,9-dione derivatives conjugated with C-protected amino acids (glycine, l-alanine, l-phenylalanine and l-glutamic acid) 6a–l were prepared by chemically modifying the prenyl substituent of 3-methyl-7-(4-methylpent-3-enyl)-1H-benzo[f]indazole-4,9-dione 2 through epoxidation, degradative oxidation, oxidation and N-acyl condensation reactions. The chemical structures of the synthesized compounds were elucidated by analyzing their IR, 1H-NMR and 13C-NMR spectral data together with elemental analysis for carbon, hydrogen and nitrogen. The preliminary in vitro antiproliferative activity of the synthesized derivatives was evaluated on KATO-III and MCF-7 cell lines using a cell proliferation assay. The majority of the derivatives exhibited significant antiproliferative activity with IC50 values ranging from 25.5 to 432.5 μM. These results suggest that 1H-benzo[f]indazole-4,9-dione derivatives are promising molecules to be researched for developing new anticancer agents.