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A series of naphthalen-1-yl-acetic acid benzylidene/(1-phenyl-ethylidene)-hydrazides (1-36) was synthesized and tested, in vitro, for antiviral, antibacterial and antifungal activities. The antibacterial and antifungal screening results indicated that compounds having o-bromo, methoxy and hydroxy substitutents were the most active ones. The results of antiviral evaluation showed that none of the synthesized derivatives inhibited the viral infection at subtoxic concentrations. QSAR investigations revealed that the multi-target QSAR model was more effective in describing the antimicrobial activity than the one-target QSAR models. Further, it revealed the importance of the partition coefficient (log P) followed by energies of the highest occupied molecular orbital (HOMO) and topological parameters, molecular connectivity indices (1χ, 3χ and 3χv) in describing the antimicrobial activity of substituted hydrazides.

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The diphosphates of a series of 2'-O-allyl-1-beta-D-arabinofuranosyl derivatives, previously obtained by us, have been prepared and tested for their inhibitory activity in an in vitro assay using R1 and R2 subunits of the purified recombinant mouse ribonucleotide reductase (RNR). 2'-O-Allyl-araU diphosphate proved to be inhibitory, with an IC50 of 100 microM. The 5'-phosphoramidate pronucleotide of 2'-O-allyl-araU was also prepared and tested for inhibition of tumor cell proliferation.

At present more than 70 human papillomaviruses (HPV) genotypes have been described and each shows a predilection for a cutaneous or mucosal surface. There is a strong association between infection with specific genital viruses (i.e., types 16 and 18) and the development of cervical cancer. Thus, intervention with the natural history of HPV infection in the genital tract may form the basis for an effective anticancer strategy. We have shown that treatment of cell lines derived from human cervical carcinomas [i.e., SiHa and CaSki (HPV-16-positive)] and HeLa (HPV-18-positive)] with HPMPC (cidofovir) results in a concentration- and time-dependent inhibition of cell proliferation. We report here the effects of HPMPC on the growth of cervical carcinoma (SiHa) xenografts in athymic nude mice. Athymic mice between the age of 6 and 8 weeks were injected SC with 5 to 10x10(6) cells. Once tumors were established, the mice were injected with PBS (placebo), HPMPC, or cytarabine (AraC) at the tumor site. Animals that were injected intratumorally with HPMPC at a dose of 5 mg/ml (0.25 mg/injection) or 10 mg/ml (0.5 mg/injection) three or five times per week, once daily, during 4 weeks showed a statistically significant reduction in tumor size compared to the placebo group or AraC group. However, when HMPC was administered topically (as a cream) or systemically (intraperitoneally), no reduction of tumor growth was observed at nontoxic concentrations, suggesting that a high local concentration of HPMPC is required to achieve a significant decrease of tumor growth.

Systemic or topical treatment with E-5-(2-bromovinyl)2'-deoxyuridine (BVDU) showed significant efficacy against orofacial infection with herpes simplex virus type 1 (HSV-1) in hairless mice. The chemotherapeutic response to BVDU was dose-dependent and clearly evident even when the treatment was initiated during the clinical manifestation of HSV-1 infection at 72 hr after inoculation. Early initiation of therapy with BVDU at 3 or 24 hr after inoculation significantly prevented the establishment of latent HSV infection in the trigeminal ganglia of mice, but systemic treatment with BVDU did not influence already established latent HSV-1. The chemotherapeutic efficacy of BVDU was comparable to that of acyclovir in the present animal model.