Synthesis of chalcone and fused rhodanine derivatives of biphosphonates active as anti-inflammatory and over breast cancer
Journal Title: Innovations in Pharmaceuticals and Pharmacotherapy (IPP) - Year 2017, Vol 5, Issue 1
Abstract
There has been considerable interest for medicinal chemist in development of a promising target for new drug development. Rhodanine, thiazolidinedione (TZD) family pharmacophore, is with diverse biological activity. Chalcones are natural products belonging to flavanoid family possessed anti-cancer and anti-inflammatory activities. Phosphonates and phosphonic acids represent an important class of organophosphorus compounds. Substitutions with P-C-P linkage of the bisphosphonates can lead to extensive alterations in their physicochemical, biological, therapeutic and toxicological characteristics. Considering this biological importance, it was aimed to synthesize a novel target which comprises the bisphosphonic acid and chalcone nucleuses with fused Rhodanine. Total 3 derivatives were synthesized and screened for InVitro cytotoxic assay on MCF-7 cell line (Breast Cancer) as well as for anti-inflammatory In-Vivo activity by carageenan induced Rat Paw Edema Method. The synthesized compounds were confirmed by physiochemical and spectral data. Among all 3 synthesized derivatives 1 st showed potent inhibition of inflammation when compared with Indomethacin as standard and promising results when screened over MCF-7 cell line against Letrozole.
Authors and Affiliations
Akhil Nagar
Keywords
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