Exploration of the effects of linker chain modifications on anti-HIV activities in a series of cosalane analogues

Transport of Cosalane—A Highly Lipophilic Novel Anti‐HIV Agent—Across Caco‐2 Cell Monolayers

“…Cosalane (NSC 658586; Figure 1) is a potent inhibitor of HIV replication with a broad range of activity against a variety of HIV‐1 isolates, HIV‐2, Rauscher murine leukemia virus, HSV‐1, HSV‐2, and human cytomegalovirus 1–5. It acts primarily by inhibiting the binding of gp120 to CD4, as well as by inhibiting a post‐attachment event prior to reverse transcriptase action 1.…”

Correlation of Anti-HIV Activity with Anion Spacing in a Series of Cosalane Analogues with Extended Polycarboxylate Pharmacophores

“…The general decrease in antiviral activity accompanying the reduction of the double bond in the linker chain is consistent with the previously reported activity of cosalane (1) vs HIV-1 RF in CEM-SS cells (EC 50 : 5.1 µM) in comparison with the activity of dihydrocosalane (31) (EC 50 : 20 µM) in the same system. 9 Overall, the data show that the conformational restriction provided by the double bond does contribute to the antiviral activity.…”

Binding of cosalane—a novel highly lipophilic anti-HIV agent—to albumin and glycoprotein

“…The primary mechanism of action appears to involve inhibition of gp 120 to CD4 binding and inhibition of post attachment event(s) prior to reverse transcription 1. The compound also demonstrated the ability to inhibit enzymatic activities of HIV‐1 reverse transcriptase and HIV protease 1,2. It is a potent inhibitor of various laboratory strains of HIV isolates, including drug resistant and clinical HIV isolates 1–3…”