[Summarizing of medicinal alerts in Ivory Coast from 2001 till 2010]. / Bilan d'une décennie d'alertes médicamenteuses en Côte d'Ivoire de 2001 à 2010.

UNLABELLED: STUDY'S AIM: This study aims a more efficient follow-up of the safety of medicines with human usage on the Ivory Coast territory. METHOD: The structure responsible for pharmacovigilance in Ivory Coast i.e. DPM listed the medicinal alerts from 2001 till 2010. RESULTS: It emerges 237 medicinal alerts among which 145 stops of marketing, 55 withdrawals of lots, 33 information notes and 4 levying of suspension of medicines. These alerts result mainly from pharmaceutical companies (49%) and the French Drug Agency or ANSM (ex-Afssaps) (43%). They mainly concern drugs of infectious target (22%) and pneumology (18%) and their motivations are so much industrial with mainly commercial reasons (27%) as of pharmacovigilance dominated by unfavorable profit/risk connections. CONCLUSION: These results constitute an important database for the survey of the medicines market in Ivory Coast and an additional motivation to accelerate the implementation of a real national center of pharmacovigilance.

[Not Available]. / Bilan d'une décennie d'alertes médicamenteuses en Côte d'Ivoire de 2001 à 2010.

STUDY'S AIM: This study aims a more efficient follow-up of the safety of medicines with human usage on the Ivory Coast territory. METHOD: The structure responsible for pharmacovigilance in Ivory Coast i.e. DPM listed the medicinal alerts from 2001 till 2010. RESULTS: It emerges 237 medicinal alerts among which 145 stops of marketing, 55 withdrawals of lots, 33 information notes and 4 levying of suspension of medicines. These alerts result mainly from pharmaceutical companies (49%) and the French Drug Agency or ANSM (ex-Afssaps) (43%). They mainly concern drugs of infectious target (22%) and pneumology (18%) and their motivations are so much industrial with mainly commercial reasons (27%) as of pharmacovigilance dominated by unfavorable profit/risk connections. CONCLUSION: These results constitute an important database for the survey of the medicines market in Ivory Coast and an additional motivation to accelerate the implementation of a real national center of pharmacovigilance.

Design and preparation of aza-analogues of benzo[c]phenanthridine framework with cytotoxic and antiplasmodial activities.

Benzo[c]phenanthridine alkaloids represent interesting lead for the discovery of new potential antiplasmodial and/or anticancer drugs. In this field, a novel library of aza-analogs of benzo[c]phenanthroline framework derivatives was designed and prepared. Although these compounds did not have specific antiplasmodial activities, some of them displayed specific in vitro activity against two cancer lines especially compound 24 with an IC(50) against the MCF7 line of 0.6 microM.

Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework.

A series of primaquine analogs was prepared, according to a conformationally restricted conformation of primaquine. In vitro antiplasmodial activities were evaluated and showed that all compounds were active on different strains of Plasmodium falciparum. In particular compounds 5 and 15 possessing a methoxy group were more active than was primaquine. Furthermore, analog 5 displayed good in vitro gametocytocidal activity. In addition selectivity indexes were calculated in respect with cytotoxic activities on Vero cell lines.

Synthesis and biological evaluation of indoloquinolines and pyridocarbazoles: a new example of unexpected photoreduction accompanying photocyclization.

Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary N-substituted enaminones derived from 1,3-cyclohexandione and 3 or 6-aminoquinoline. The angular cyclized compounds thus obtained were tested in vitro on K 562 cells and A 2780 doxorubicin sensitive and resistant cells. All compounds were less effective than doxorubicin in sensitive cells but their activity wasn't decreased by MDR resistance.

In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.

A series of trisubstituted 1,10-phenanthrolines was prepared. These compounds exhibited mild to high biological activities in vitro both toward chloroquino-resistant FcB1-Columbia and FcM29-Cameron strains and Nigerian chloroquino-sensitive strain of Plasmodium falciparum. Cytotoxicity of the most active compounds was estimated showing that one compound (10) exhibited a selective activity against malaria parasite (selectivity indexes of 52 and 144). Antiplasmodial activity of this derivative was optimized by N-10 alkylation and the phenanthrolinium salt (15) submitted to an in vivo study using mice infected by P. vinckei petteri showing an ED50 of 7.86 mg/kg/day.

A photochemical approach to pyridopyrroloquinoline derivatives as new potential anticancer agents.

Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developped a synthesis based on the photocyclisation of tertiary N-methylated enaminones derived from cyclopentane-1,3-dione and 3 or 6-aminoquinoline. The angular cyclised compounds thus obtained were submitted to Beckmann rearrangement, preceded by the formation of a Z oxime. Finally, the delta-lactame ring was oxidized using 10% palladium/carbon in diphenylether and pyridopyrroloquinolines were obtained. These compounds and the intermediate lactams and cyclopentanopyrroloquinolines were tested in vitro on K 562 cells and A 2780 doxorubicine sensitive and resistant cells. All compounds were less effective than doxorubicine in sensitive cells but their activity wasn't decreased by MDR resistance.