Inhibitory effect of novel S,N-bisphosphonates on some carcinoma cell lines, osteoarthritis, and chronic inflammation

A new series of S,N-bisphosphonate derivatives was synthesized and evaluated as antitumor agents against breast-, cervix-, liver, and colon cancer diseases. Antiarthritic and antichronic inflammatory properties of the new bisphosphonates (BPs) were also investigated. The studies demonstrated an efficient site selective method for making condensation products of BP-derivatives in high yields from thiazinethiones and tetraethyl methylenebisphosphonate reagent. The bioscreening evaluation showed that one of the tested BPs exhibited remarkable antitumor activity against the four tested carcinoma cell lines; nevertheless, all tested S,N-BP-derivatives (11 compounds) showed significant to moderate anti-inflammatory activity and capable of inhibiting polyarthritis.

Graphical AbstractA new series of S,N-bisphosphonate derivatives was synthesized and evaluated as antitumor agents against breast cancer, cervix, liver, and colon. Antiarthritic and antichronic inflammatory properties of the new bisphosphonates were investigated.Figure optionsDownload as PowerPoint slideHighlights
► Condensation reactions of thiazinethiones with methylenebisphosphonate reagent.
► Synthesis of a new series of S, and N-bisphosphonates and relevant acids.
► The new bisphosphonates showed potency against four carcinoma cell lines.
► Four out of eleven tested bisphosphonates capable of inhibiting polyarthritis.
► All tested S,N-bisphosphonates showed significant to moderate anti-inflammatory activity.