HASSAN M. OTIFI¹, MISHARI ALSHYARBA², MAJED AL FAYI^3,4, AYED A. DERA^3,4, PRASANNA RAJAGOPALAN^3,4,*

Oncology Research, Vol.29, No.3, pp. 217-227, 2021, DOI:10.32604/or.2022.03570 - 01 August 2022

Abstract Targeted therapies are gaining global attention to tackle Renal Cancer (RC). This study aims to screen FPMXY- 14 (novel arylidene analogue) for Akt inhibition by computational and in vitro methods. FPMXY-14 was subjected to proton NMR analysis and Mass spectrum analysis. Vero, HEK-293, Caki-1, and A498 cell lines were used. Akt enzyme inhibition was studied with the fluorescent-based kit assay. Modeller 9.19, Schrodinger 2018-1, LigPrep module, and Glide docking were used in computational analysis. The nuclear status was assessed by PI/Hoechst- 333258 staining, cell cycle, and apoptosis assays were performed using flow cytometry. Scratch wound and… More >

Prasanna Rajagopalan^*†, Abdulrahim Hakami^*†, Mohammed Ragab^*, Ashraf Elbessoumy^*‡

Oncology Research, Vol.27, No.8, pp. 957-964, 2019, DOI:10.3727/096504019X15555428221646

Abstract Arylidene analogs are well proven for biological activities. FCY-302, a novel small molecule belonging to this class, was screened for its biological efficacy in leukemia and myeloma cells. FCY-302 selectively inhibited proliferation of cancer cells with GI50 values of 395.2 nM, 514.6 Nm, and 642.4 nM in HL-60, Jurkat, and RPMI-8226 cells, respectively. The compound also increased sub-G0 peak in the cancer cell cycle and favored apoptosis determined by annexin V assay. The compound decreased the antiapoptotic Bcl-2 levels and increased proapoptotic Bax proteins in leukemia and myeloma cell lines. FCY-302 attenuated the mitochondrial membrane-bound Na⁺ More >