3-Alkenyl-2-oxindoles: Synthesis, antiproliferative and antiviral properties against SARS-CoV-2

Abstract

Graphical abstract Sets of 3-alkenyl-2-oxindoles were synthesized of potential antiproliferative (against PaCa-2 and MCF7cancer cell lines) and promising properties against SARS-CoV-2.

Synthesis of aspirin-curcumin mimic conjugates of potential antitumor and anti-SARS-CoV-2 properties

“…The standard MTT bioassay technique was considered for antiproliferation properties determination of the synthesized agents 5a–p [79] . Table 1 displays the IC 50 (concentration capable for 50% growth inhibition of the tested cell line) of the synthesized agents 5a–p and reference standards (5-fluorouracil and sunitinib) which are clinically approved drugs against the considered cancer cell lines (Supplementary Figs.…”

“…Flow cytometric analysis is an accessible and rapid technique used intensively in medicinal chemical studies for assigning the cell cycle progress of living cells. The detected fluorescence levels estimate quantitatively the DNA content hence; determine the progress of cell cycle [79] , [84] . Compounds 5c and 5o (the most promising agents synthesized with high potency against HCT116) were selected for flow cytometric analysis studies applying the IC 50 value of each respective agent observed through MTT bio-assay, to identify their impact on the progress of cell cycle and accessibility for induction of apoptosis and/or necrosis.…”

“…The anti-SARS-CoV-2 properties of the synthesized aspirin-curcumin mimic conjugates were determined by the standard technique ( Table 4 , Fig. 6 ) [79] , [85] , [86] . Generally, all the synthesized agents (compounds 5c , 5f and 5j are exceptions) show potent anti-SARS-CoV-2 properties (IC 50 = 1.659-8.828 µ M) relative to the standard references used (IC 50 = 36.92, 24.98 µ M for hydroxychloroquine and chloroquine, respectively).…”

“…Molecular docking studies were undertaken for validation the EGFR properties of the synthesized conjugates utilizing Discovery Studio 2.5 software (CDOCKER standard technique) [79] , [113] . Adoption of the EGFR properties for computational studies, are due to the promising observations revealed relative to the exhibited VEGFR-2 properties.…”

Thyroid Cancer and COVID-19: Prospects for Therapeutic Approaches and Drug Development

“…Girgis et al. performed chemical modifications of sunitinib, then verified the antiviral properties of the products against SARS-CoV-2; they reported that sunitinib may be effective for the treatment of COVID-19 ( 99 ). Zhang et al.…”